UNC5293

发表于2024年10月29日由上海金畔生物科技有限公司

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

UNC5293 纯度: 99.31%

UNC5293 是一种 MERTK 选择性的有效抑制剂 (K_i=190 pM)。UNC5293 抑制 MERTK (IC₅₀=0.9 nM)，对 Axl、Tyro3 和 Flt3 更具选择性。UNC5293 表现出优异的小鼠药代动力学特性，并可以被用于骨髓白血病研究。

UNC5293 Chemical Structure

CAS No. : 2226789-82-6

规格	价格	是否有货
5 mg	￥4800	In-stock
10 mg	￥8000	In-stock
25 mg	￥16500	In-stock
50 mg	￥26000	In-stock
100 mg	￥40000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

UNC5293 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Kinase Inhibitor Library
Protein Tyrosine Kinase Compound Library
Anti-Cancer Compound Library
Anti-Lung Cancer Compound Library
Anti-Blood Cancer Compound Library

生物活性

UNC5293 is a MERTK-selective and potent inhibitor (K_i=190 pM). UNC5293 inhibits MERTK (IC₅₀=0.9 nM) and is more selective over Axl, Tyro3 and Flt3. UNC5293 exhibits excellent mouse PK properties and is used for bone marrow leukemia research^[1].

IC₅₀ & Target

Ki: 190 pM (MERTK)
IC50: 0.9 nM (MERTK)^[1]

体外研究
(In Vitro)

UNC5293 provides selective target inhibition in cell-based assays. In cultures of the human B-cell acute lymphoblastic leukemia (B-ALL) cell line, UNC5293 inhibits phosphorylation of MERTK with an IC₅₀ of 9.4 nM. In the SEM B-ALL cell line, UNC5293 is less potent against FLT3, with an IC₅₀ of 170 nM^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

UNC5293 (oral administration; 120 mg/kg; single dose) effectively inhibit MERTK in vivo in orthotopic 697 B-ALL mice xenografts^[1].
UNC5293 (oral gavage; 3 mg/kg; single dose) has excellent mouse PK properties (7.8 h half-life and 58% oral bioavailability), and the C_max and AUC_last are 9.2 μM and 2.5 h*μM, respectively^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

518.69

Formula

C₃₀H₄₂N₆O₂

CAS 号

2226789-82-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

In Vitro:

DMSO : 100 mg/mL (192.79 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9279 mL	9.6397 mL	19.2793 mL
5 mM	0.3856 mL	1.9279 mL	3.8559 mL
10 mM	0.1928 mL	0.9640 mL	1.9279 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (4.82 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.82 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (4.82 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.82 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.82 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.82 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Hongchao Zheng, et al. UNC5293, a potent, orally available and highly MERTK-selective inhibitor. Eur J Med Chem. 2021 May 17;220:113534.

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UNC 0631

发表于2024年10月20日由上海金畔生物科技有限公司

UNC 0631 纯度: 99.35%

UNC 0631 是一种有效的组蛋白甲基转移酶 G9a 抑制剂，IC₅₀ 值为 4 nM。UNC 0631 有效降低 MDA-MB-231 细胞中 H3K9me2 的水平，IC₅₀ 为 25 nM。

UNC 0631 Chemical Structure

CAS No. : 1320288-19-4

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1497	In-stock
5 mg	￥1070	In-stock
10 mg	￥1860	In-stock
25 mg	￥3980	In-stock
50 mg	￥6315	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

UNC 0631 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Anti-Blood Cancer Compound Library

生物活性

UNC 0631 is a potent histone methyltransferase G9a inhibitor with an IC₅₀ of 4 nM. UNC 0631 potently reduces H3K9me2 levels in MDA-MB-231 cells with an IC₅₀ of 25 nM^[1].

IC₅₀ & Target

G9a

4 nM (IC₅₀)

体外研究
(In Vitro)

UNC 0631 (Compound 7) has high cellular potency and excellent separation of functional potency versus cell toxicity in a variety of cell lines. UNC 0631 is highly potent in reducing H3K9me2 levels and has low cell toxicity. UNC 0631 reduces H3K9me2 levels with ICW IC₅₀ values of 25 nM, 18 nM, 26 nM, 24 nM, 51 nM, 72 nM and 46 nM in MDA-MB-231, MCF7, PC3, 22RV1, HCT116 wt, HCT 116 p53^-/- and IMR90 cell lines, respectively^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

635.93

Formula

C₃₇H₆₁N₇O₂

CAS 号

1320288-19-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMF : 150 mg/mL (235.88 mM; Need ultrasonic)

Ethanol : 100 mg/mL (157.25 mM; Need ultrasonic)

DMSO : 16.67 mg/mL (26.21 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5725 mL	7.8625 mL	15.7250 mL
5 mM	0.3145 mL	1.5725 mL	3.1450 mL
10 mM	0.1573 mL	0.7863 mL	1.5725 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% EtOH 40% PEG300 5% Tween-80 45% saline

Solubility: 2.5 mg/mL (3.93 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (3.93 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% EtOH 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (3.93 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.93 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% EtOH 90% corn oil

Solubility: ≥ 2.5 mg/mL (3.93 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.93 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 900 μL玉米油中，混合均匀。
4.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 1.67 mg/mL (2.63 mM); Clear solution

此方案可获得 ≥ 1.67 mg/mL (2.63 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
5.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 1.67 mg/mL (2.63 mM); Clear solution

此方案可获得 ≥ 1.67 mg/mL (2.63 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Liu F, et al. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J Med Chem. 2011 Sep 8;54(17):6139-50.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

UNC3230

发表于2024年10月19日由上海金畔生物科技有限公司

UNC3230 纯度: 99.93%

UNC3230 是一种有效的选择性的,ATP 竞争性的磷脂酰肌醇 4 磷酸 5 激酶 1C 型 (PIP5K1C) 抑制剂，IC₅₀ 约为 41 nM。UNC3230 还可抑制 PIP4K2C，但不抑制其他调节磷酸肌醇水平的脂质激酶。UNC3230 具有缓解疼痛和抗癌作用。

UNC3230 Chemical Structure

CAS No. : 1031602-63-7

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1430	In-stock
5 mg	￥1300	In-stock
10 mg	￥2000	In-stock
50 mg	￥7000	In-stock
100 mg	￥9800	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

UNC3230 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Immunology/Inflammation Compound Library
Kinase Inhibitor Library
Anti-Cancer Compound Library
Targeted Diversity Library

生物活性

UNC3230 is a potent, selective and ATP-competitive PIP5K1C inhibitor with an IC₅₀ of ~41 nM. UNC3230 also inhibits PIP4K2C and does not inhibit any of the other lipid kinases that regulate phosphoinositide levels. UNC3230 has antinociceptive and anticancer effects^[1].

IC₅₀ & Target

IC50: ~41 nM (Phosphatidylinositol 4-phosphate 5 kinase type 1C (PIP5K1C))^[1]

体外研究
(In Vitro)

Membrane PIP2 levels are significantly reduced by ~45% in dorsal root ganglia (DRG) neurons treated with 100 nM UNC3230 (~2-fold above the IC50) relative to vehicle controls. UNC3230 significantly reduces lysophosphatidic acid (LPA)-evoked calcium signaling in cultured DRG neurons relative to vehicle^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

UNC3230 (2 nmol) significantly increases noxious heat-evoked paw withdrawal latency for two hours after intrathecal injection in wild-type mice, indicating an antinociceptive effect^[1].
UNC3230 (2 nmol; intrathecal injection) is administered then one hour later co-injected 1 nmol LPA with UNC3230 (2 nmol, intrathecal injection). UNC3230 significantly blunts thermal hyperalgesia and mechanical allodynia compared to vehicle^[1].
UNC3230 (2 nmol; intrathecal injection) significantly blunts thermal hyperalgesia and mechanical allodynia in the complete Freund’s adjuvant (CFA)-inflamed hindpaw (relative to vehicle control) but does not affect thermal or mechanical sensitivity in the control (non-inflamed) hindpaw over a multiday time course^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

344.43

Formula

C₁₇H₂₀N₄O₂S

CAS 号

1031602-63-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 125 mg/mL (362.92 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.9033 mL	14.5167 mL	29.0335 mL
5 mM	0.5807 mL	2.9033 mL	5.8067 mL
10 mM	0.2903 mL	1.4517 mL	2.9033 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (6.04 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.04 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Wright BD, et al. The lipid kinase PIP5K1C regulates pain signaling and sensitization. Neuron. 2014 May 21;82(4):836-47.

[2]. Peng W, et al. Type Iγ phosphatidylinositol phosphate kinase promotes tumor growth by facilitating Warburg effect in colorectal cancer. EBioMedicine. 2019 Jun;44:375-386.

[3]. Wright BD, et al. Development of a High-Throughput Screening Assay to Identify Inhibitors of the Lipid Kinase PIP5K1C. J Biomol Screen. 2015 Jun;20(5):655-62.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

UNC3866

发表于2024年10月16日由上海金畔生物科技有限公司

UNC3866 纯度: 97.14%

UNC3866 是一种有效的 CBX7-H3 拮抗剂，IC₅₀ 为 66±1.2 nM。

UNC3866 Chemical Structure

CAS No. : 1872382-47-2

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1836	In-stock
2 mg	￥800	In-stock
5 mg	￥1200	In-stock
10 mg	￥2100	In-stock
25 mg	￥3900	In-stock
50 mg	￥7500	In-stock
100 mg	￥13500	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

UNC3866 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Peptidomimetic Library
Reprogramming Compound Library
Chemical Probe Library
Anti-Blood Cancer Compound Library
Targeted Diversity Library

生物活性

UNC3866 is a potent antagonist of the CBX7-H3 interaction as determined by AlphaScreen (IC₅₀=66±1.2 nM) and is more than 100-fold selective for CBX7 over the other nine members of this methyl-lysine (Kme) reader panel.

IC₅₀ & Target

IC50: 66±1.2 nM (CBX7)^[1]

体外研究
(In Vitro)

UNC3866, a potent antagonist of the methyl-lysine (Kme) reading function of the Polycomb CBX and CDY families of chromodomains. UNC3866 binds the chromodomains of CBX4 and CBX7 most potently with a K_d of 100 nM for each, and is 6- to 18-fold selective versus seven other CBX and CDY chromodomains while being highly selective versus >250 other protein targets. UNC3866 inhibits PC3 cell proliferation, a known CBX7 phenotype, while UNC4219, a methylated negative control compound, has negligible effects. UNC3866 is a potent and cellularly active antagonist of PRC1 chromodomains. UNC3866 is the most potent ligand reported for CBX7 with a K_d of 97±2.4 nM. UNC3866 is equipotent for CBX4, which is most similar to CBX7, while it is 18-, 6- and 12-fold selective for CBX4/7 over CBX2, -6 and -8, respectively. Additionally, UNC3866 is 65-fold selective for CBX4/7 over CDY1 and 9-fold selective for CBX4/7 over CDYL1b and CDYL2^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

795.02

Formula

C₄₃H₆₆N₆O₈

CAS 号

1872382-47-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 27 mg/mL (33.96 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.2578 mL	6.2891 mL	12.5783 mL
5 mM	0.2516 mL	1.2578 mL	2.5157 mL
10 mM	0.1258 mL	0.6289 mL	1.2578 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (3.14 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.14 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (3.14 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.14 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (3.14 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.14 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Stuckey JI, et al. A cellular chemical probe targeting the chromodomains of Polycomb repressive complex 1. Nat Chem Biol. 2016 Mar;12(3):180-7.

Kinase Assay ^[1]	The effect of UNC3866 on the methyltransferase activity of G9a, EHMT1, SUV39H1, SUV39H2, SETDB1, SETD8, SUV420H1, SUV420H2, SETD7, MLL1 trimeric complex, MLL3 tetrameric complex, EZH2 trimeric complex, PRMT1, PRMT3, PRMT5-MEP50 complex, PRMT6, PRMT7, PRMT8, PRDM9, SETD2, SMYD2, SMYD3, BCDIN3D and DNMT1 is assessed by monitoring the incorporation of tritium-labeled methyl group to lysine or arginine residues of peptide substrates using Scintillation Proximity Assay (SPA). Assays are performed in a 20 μL reaction mixture containing ³H-SAM at substrate concentrations close to the K_m values for each enzyme. Three concentrations (1 μM, 10 μM, and 50 μM) of UNC3866 are used in all selectivity assays. To stop the enzymatic reactions, 7.5 M Guanidine hydrochloride is added, followed by 180 μL of buffer (20 mM Tris, pH 8.0). The reactions are mixed and then transferred to a 96-well FlashPlate. The reaction mixtures in Flash plates are incubated for 1 hour and the CPM are measured using a TopCount plate reader. The CPM counts in the absence of compound for each data set are defined as 100% activity. In the absence of the enzyme, the CPM counts in each data set are defined as background (0%)^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	PC3 cells are seeded at 200 cells/well into 24-well plates. Cells are allowed to adhere overnight. The media (DMEM supplemented with 10 % FBS) is then exchanged with fresh media containing DMSO, UNC3866 or UNC4219. On day three, the media are exchanged with fresh media containing DMSO, UNC3866 or UNC4219. For dose-response studies, the EC₅₀ is derived from a six-point titration ranging from 100 μM to 0.4 μM of UNC3866 or UNC4219. At day 0, 3 or 6, cells are fixed with ice-cold methanol for 30 sec. and rehydrated with PBS. Nuclei of the cells are stained with DAPI (0.05 μg/mL) and numerated using High Content Microscopy. For dose-response studies, the cell count of UNC3866- or UNC4219-treated cells is normalized to the average cell count of DMSO-treated cells. The EC₅₀ is calculated using the “log[inhibitor] vs. the normalized response-Variable slope” equation in GraphPad Prism 5^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Stuckey JI, et al. A cellular chemical probe targeting the chromodomains of Polycomb repressive complex 1. Nat Chem Biol. 2016 Mar;12(3):180-7.

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UNC0642

发表于2024年10月6日由上海金畔生物科技有限公司

UNC0642 纯度: 99.82%

UNC0642是有效，选择性的赖氨酸甲基转移酶 G9a 和 GLP 抑制剂，抑制 G9a 的IC₅₀ 值小于2.5 nM。

UNC0642 Chemical Structure

CAS No. : 1481677-78-4

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1082	In-stock
5 mg	￥900	In-stock
10 mg	￥1500	In-stock
50 mg	￥4500	In-stock
100 mg	￥8500	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

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Bioactive Compound Library Plus
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生物活性

UNC0642 is a potent and selective lysine methyltransferases G9a and GLP inhibitor, with an IC₅₀ of <2.5 nM for G9a.

IC₅₀ & Target

IC50: <2.5 nM (G9a)^[1]

体外研究
(In Vitro)

UNC0642 displays high in vitro and cellular potency, low cell toxicity, and excellent selectivity. UNC0642 is competitive with the peptide substrate and non-competitive with the cofactor SAM. The K_i of UNC0642 is determined to be 3.7±1 nM. UNC0642 displays high in vitro potency for GLP (IC₅₀< 2.5 nM), similar to G9a. UNC0642 is more than 300-fold selective for G9a and GLP over a broad range of kinases, GPCRs, transporters, and ion channels. UNC0642 exhibits high potency at reducing the H3K9me2 mark, low cell toxicity, and good separation of functional potency and cell toxicity in a number of cell lines. It reduces clonogenicity in PANC-1 cells, a pancreatic carcinoma cell line^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

A single intraperitoneal (IP) injection (5 mg/kg) of UNC0642 results in a plasma C_max (maximum concentration) of 947 ng/mL and an AUC (area under the curve) of 1265 hr*ng/mL^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

546.70

Formula

C₂₉H₄₄F₂N₆O₂

CAS 号

1481677-78-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 50 mg/mL (91.46 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8292 mL	9.1458 mL	18.2916 mL
5 mM	0.3658 mL	1.8292 mL	3.6583 mL
10 mM	0.1829 mL	0.9146 mL	1.8292 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.57 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.57 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.57 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Liu F, et al. Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. J Med Chem. 2013 Nov 14;56(21):8931-8942.

[2]. Wang L, et al. Targeting EHMT2 reverses EGFR-TKI resistance in NSCLC by epigenetically regulating the PTEN/AKT signaling pathway. Cell Death Dis. 2018 Jan 26;9(2):129

Cell Assay ^[1]	MDA-MB-231, PC3, and U2OS cells are treated with inhibitors (UNC0642) for 48 h. Cell viability assays are performed by incubating cells with 0.1 mg/mL of resazurin for 3 – 4 h. Resazurin reduction is monitored with 544 nm excitation, measuring fluorescence at 590 nm. In-cell western assay is performed as described previously^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice: Standard PK studies are performed using male Swiss albino mice. Plasma and brain concentrations are measured at 0.08, 0.25, 0.5, 1, 2, 4, 8, and 24 h following a single IP injection of UNC0642 at 5 mg/kg. The compound concentration at each time point in plasma or brain is the average value from 3 test animals^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Liu F, et al. Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. J Med Chem. 2013 Nov 14;56(21):8931-8942. [2]. Wang L, et al. Targeting EHMT2 reverses EGFR-TKI resistance in NSCLC by epigenetically regulating the PTEN/AKT signaling pathway. Cell Death Dis. 2018 Jan 26;9(2):129

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UNC2250

发表于2024年10月6日由上海金畔生物科技有限公司

UNC2250 纯度: 99.22%

UNC2250 是一种有效选择性的 Mer 抑制剂，IC₅₀为 1.7 nM，比相关的激酶 Axl 和 Tyro3 选择性高 160 倍和 60 倍。

UNC2250 Chemical Structure

CAS No. : 1493694-70-4

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥798	In-stock
5 mg	￥725	In-stock
10 mg	￥1200	In-stock
50 mg	￥4241	In-stock
100 mg	￥7400	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

UNC2250 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Kinase Inhibitor Library
Protein Tyrosine Kinase Compound Library
Anti-Cancer Compound Library
Anti-Lung Cancer Compound Library
Targeted Diversity Library

生物活性

UNC2250 is a potent and selective Mer inhibitor with an IC₅₀ of 1.7 nM, about 160- and 60-fold selectivity over the closely related kinases Axl/Tyro3.

IC₅₀ & Target

IC50: 1.7 nM (Mer)^[1]

体外研究
(In Vitro)

UNC2250 (5-500 nM; 1 hour) inhibits Mer phosphorylation in 697 B-ALL cells with an IC₅₀ value of 9.8 nM^[1].
UNC2250 efficiently inhibits ligand-dependent phosphorylation of a chimeric protein consisting of the extracellular and transmembrane domains of the epidermal growth factor (EGF) receptor and the intracellular tyrosine kinase domain of Mer^[1].
UNC2250 incubation inhibits colony formation in soft agar cultures of the BT-12 rhabdoid tumor and the Colo699 NSCLC cell lines^[1] .

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:	697 B-ALL cells
Concentration:	5, 10, 20, 50, 100, 250, 500 nM
Incubation Time:	1 hour
Result:	Inhibits Mer phosphorylation in 697 B-ALL cells with an IC₅₀ value of 9.8 nM.

分子量

440.58

Formula

C₂₄H₃₆N₆O₂

CAS 号

1493694-70-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 20 mg/mL (45.39 mM; ultrasonic and warming and heat to 60°C)

0.1 M HCL : 12.5 mg/mL (28.37 mM; ultrasonic and adjust pH to 3 with HCl)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2697 mL	11.3487 mL	22.6974 mL
5 mM	0.4539 mL	2.2697 mL	4.5395 mL
10 mM	0.2270 mL	1.1349 mL	2.2697 mL

参考文献

[1]. Zhang, W., et al., Pseudo-cyclization through intramolecular hydrogen bond enables discovery of pyridine substituted pyrimidines as new Mer kinase inhibitors. J Med Chem, 2013. 56(23): p. 9683-92.

[2]. Xiaodong Wang, et al. Pyrimidine compounds for the treatment of cancer.WO2013177168A1.

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UNC1999

发表于2024年10月5日由上海金畔生物科技有限公司

UNC1999 纯度: 99.85%

UNC1999 是一种有效，选择性和SAM-竞争性的 EZH2 和 EZH1 抑制剂，IC₅₀ 分别为 <10 nM 和 45 nM。

UNC1999 Chemical Structure

CAS No. : 1431612-23-5

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥895	In-stock
5 mg	￥714	In-stock
10 mg	￥1116	In-stock
50 mg	￥3348	In-stock
100 mg	￥5990	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

UNC1999 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Autophagy Compound Library
Reprogramming Compound Library
Chemical Probe Library
Anti-Blood Cancer Compound Library

生物活性

UNC1999 is a SAM-competitive, potent and selective inhibitor of EZH2/1 with IC₅₀s of <10 nM and 45 nM, repectively.

IC₅₀ & Target

IC50: <10 nm (ezh2), 45 (ezh1)^[1]

体外研究
(In Vitro)

UNC1999, the first orally bioavailable inhibitor that has high in vitro potency for wild-type and mutant EZH2 as well as EZH1, a closely related H3K27 methyltransferase that shares 96% sequence identity with EZH2 in their respective catalytic domains. UNC1999 is highly selective for EZH2 and EZH1 over a broad range of epigenetic and non-epigenetic targets, competitive with the cofactor SAM, and non-competitive with the peptide substrate. UNC1999 has K_i values of 4,700 nM, 65 nM, 300 nM, and 1,500 nM for sigma1, sigma2, histamine H₃, and NET, respectively. NC1999 selectively kills DB cells, a DLBCL cell line with the EZH2 Y641N mutation. UNC1999 displays a concentration- and time-dependent inhibition of DB cell proliferation (EC₅₀=633±101 nM (n=3))^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

A single intraperitoneal (IP) injection of UNC1999 at 15, 50, or 150 mg/kg achieved high C_max (9,700-11,800 nM) and exhibited dose linearity in male Swiss albino mice. Both the 150 and 50 mg/kg IP doses resulted in the plasma concentrations of UNC1999 above its cellular IC₅₀ over the entire 24 h period while the 15 mg/kg IP dose led to the plasma concentrations of UNC1999 above its cellular IC₅₀ for approximately 12 h. We next examined whether UNC1999 is orally bioavailable and are pleased to find that a single 50 mg/kg oral dose of UNC1999 achieved high C_max (4,700 nM) and good exposure levels in male Swiss albino mice. The plasma concentrations of UNC1999 are maintained above its cellular IC₅₀ for approximately 20 h following this single oral dose. It is worth noting that all doses including the 150 mg/kg IP dose are well tolerated by all test mice, and no adverse effects are observed^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

569.74

Formula

C₃₃H₄₃N₇O₂

CAS 号

1431612-23-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL (175.52 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 80°C) (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7552 mL	8.7759 mL	17.5519 mL
5 mM	0.3510 mL	1.7552 mL	3.5104 mL
10 mM	0.1755 mL	0.8776 mL	1.7552 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.25 mg/mL (3.95 mM); Clear solution

此方案可获得 ≥ 2.25 mg/mL (3.95 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 22.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: 2.25 mg/mL (3.95 mM); Suspended solution; Need ultrasonic

此方案可获得 2.25 mg/mL (3.95 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 22.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: 2.25 mg/mL (3.95 mM); Clear solution; Need warming

此方案可获得 2.25 mg/mL (3.95 mM) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 22.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Konze KD, et al. An Orally Bioavailable Chemical Probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol. 2013;8(6):1324-34.

Kinase Assay ^[1]	EZH2 Y641N mutant is generated and assayed by BPS Bioscience. A series of dilutions of UNC1999 are prepared with 10% DMSO in HMT assay buffer and 5 μL of the dilution is added to a 50 μL reaction so that the final concentration of DMSO is 1% in all of reactions. All of the enzymatic reactions are conducted in duplicate at room temperature for 60 minutes (EZH2) and 180 minutes (EZH2 Y641N) in a 50 μL mixture containing HMT assay buffer, S-adenoslymethionine, enzyme, and UNC1999. These 50 μL reactions are carried out in wells of a HMT substrate pre-coated plate. After enzymatic reactions, the reaction mixtures are discarded and each of the wells is washed three times with TBST buffer, and slowly shaken with Blocking Buffer for 10 minutes. Wells are emptied, and 100 μL of diluted 1°antibody is added. The plate is then slowly shaken for 60 minutes at room temperature. As before, the plate is emptied and washed three times, and shaken with Blocking Buffer for 10 minutes at room temperature. After discarding the Blocking Buffer, 100 μL of diluted 2°antibody is added. The plate is then slowly shaken for 30 minutes at room temperature. As before, the plate is emptied and washed three times, and shaken with Blocking Buffer for 10 minutes at room temperature. Blocking Buffer is discarded and a mixture of the HRP chemiluminescent substrates is freshly prepared. 100 μL of this mixture is added to each empty well. Immediately, the luminescence of the samples is measured in a BioTek SynergyTM 2 microplate reader^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	DB cells, a diffuse-large B-cell lymphoma cell line harboring the EZH2 Y641N mutation, are obtained from ATCC and cultured in RPMI 1640 supplemented with 10% fetal bovine serum, antibiotics, and various concentration of UNC1999 (0.1, 0.2, 0.3, 0.4, 0.5, 1, 2, 3, and 5 μM) or UNC2400 and DMSO control. The medium containing the test compound or control is refreshed every three days. The numbers of viable cells from at least three independent experiments are measured using TC20 automated cell counter system. Total histones are prepared from cell nuclei using an acidic extraction protocol. About 1 microgram of total histones is separated using 15% of SDS-PAGE, transferred to PVDF membranes, and probed with histone antibodies. Antibodies used in this study are those against EZH2, general H3, and H3K27me3^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] Standard PK studies are conducted using male Swiss albino mice at Sai Life Sciences. Four doses (15, 50, and 150 mg/kg IP, and 50 mg/kg PO) of UNC1999 are evaluated. Each study lasted 24 h. Plasma concentrations of UNC1999 reported at each of the eight time points (0.08, 0.25, 0.5, 1, 2, 4, 8, and 24 h post dosing) are the average values from 3 test animals. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Konze KD, et al. An Orally Bioavailable Chemical Probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol. 2013;8(6):1324-34.

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MRX-2843(Synonyms: UNC2371)

发表于2024年10月4日由上海金畔生物科技有限公司

MRX-2843 (Synonyms: UNC2371) 纯度: 99.70%

MRX-2843 (UNC2371) 是一种具有口服活性的、ATP 竞争性的 MERTK 和 FLT3 酪氨酸激酶抑制剂 (TKI)，IC₅₀ 分别为 1.3 nM 和 0.64 nM。

MRX-2843 Chemical Structure

CAS No. : 1429882-07-4

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥3010	In-stock
1 mg	￥1000	In-stock
5 mg	￥2800	In-stock
10 mg	￥4800	In-stock
25 mg	￥9800	In-stock
50 mg	￥14000	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

MRX-2843 相关产品

•相关化合物库:

Drug Repurposing Compound Library Plus
Clinical Compound Library Plus
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Kinase Inhibitor Library
Protein Tyrosine Kinase Compound Library
Anti-Cancer Compound Library
Clinical Compound Library
Drug Repurposing Compound Library
Orally Active Compound Library
Anti-Blood Cancer Compound Library

生物活性

MRX-2843 (UNC2371) is an orally active, ATP-competitive dual MERTK and FLT3 tyrosine kinases inhibitor (TKI) with enzymatic IC₅₀s of 1.3 nM for MERTK and 0.64 nM for FLT3, respectively^[1].

IC₅₀ & Target

MERTK, FLT3^[1]

体外研究
(In Vitro)

In the Kasumi-1 cell line, treatment with MRX-2843 results in dose-dependent inhibition of MERTK phosphorylation. Decreased phosphorylation is evident at concentrations as low as 10 nM, with near-complete abrogation of MERTK activation at 100 to 300 nM. Similarly, treatment of Kasumi-1 cells with MRX-2843 mediates inhibition of downstream signaling through pathways important for tumor cell survival and proliferation. MRX-2843 treatment results in a decrease in relative cell numbers, with an IC₅₀ of 143.5±14.1 nM, indicating that MRX-2843 significantly inhibits tumor cell proliferation and/or survival. Similarly, there are 34.1%±5.6% and 67.1%±2.7% apoptotic and dead cells in NOMO-1 cultures treated with 150 nM or 300 nM MRX-2843, respectively, compare with 6.8%±0.7% in vehicle-treated cultures (P<0.001). Treatment with 50 nM and 100 nM MRX-2843 results in 62.3%±6.4% and 84.1%±7.8% inhibition of colony formation, respectively, in Kasumi-1 cultures (P<0.01). Similarly, in NOMO-1 cultures, colony formation is inhibited by 54.8%±18.1% in response to treatment with 100 nM MRX-2843 (P<0.001). In MOLM-14 cells, treatment with MRX-2843 inhibits phosphorylation of FLT3 and downstream signaling through STAT5, ERK1/2, and AKT. Activation of FLT3 and its signaling pathways is almost completely abrogated by treatment with 50 nM MRX-2843, indicating somewhat higher cellular potency against FLT3 relative to MERTK^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

MRX-2843 is 78% orally bioavailable at a dose of 3 mg/kg with a C_max of 1.3 μM and a t_1/2 of 4.4 hours. In MOLM-14 parental xenografts, both quizartinib and MRX-2843 increase median survival compare with that of vehicle-treated mice (172.5 days versus 40 days and 121 days versus 36 days, respectively, P<0.001). In this model, quizartinib is more effective than MRX-2843 (P<0.005), although higher doses of MRX-2843 are not evaluated. In MOLM-14:D835Y xenografts, quizartinib prolongs survival compare with that of vehicle-treated mice, but the effect is minimal (median survival 45 days vs. 36 days, P<0.001). In MOLM-14:F691L xenografts, treatment with MRX-2843 prolongs survival by almost 2-fold in NSG and NSGS mice (median survival 87 vs. 44.5 days and 87 vs. 48 days, respectively, P<0.005). Increased survival is observed in response to treatment with MRX-2843 versus quizartinib, but the difference is only significant in NSG mice^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

488.67

Formula

C₂₉H₄₀N₆O

CAS 号

1429882-07-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 31.25 mg/mL (63.95 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0464 mL	10.2319 mL	20.4637 mL
5 mM	0.4093 mL	2.0464 mL	4.0927 mL
10 mM	0.2046 mL	1.0232 mL	2.0464 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (4.26 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.26 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (4.26 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.26 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.26 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.26 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Minson KA, et al. The MERTK/FLT3 inhibitor MRX-2843 overcomes resistance-conferring FLT3 mutations in acute myeloid leukemia. JCI Insight. 2016 Mar;1(3):e85630.

Cell Assay ^[1]	Cell lines are cultured (10,000 cells/sample) in 0.35% Noble agar on a 0.5% Noble agar base layer and overlaid with cRPMI containing kinase inhibitor (including MRX-2843) or vehicle. The overlying medium is replaced 2 to 3 times per week, and vehicle treatment is assessed in duplicate. After 14 days or 21 days (Kasumi-1 cells only), colonies are stained with 1 mg/mL nitrotetrazolium blue for 4 hours and counted using a colony counter. Mononuclear cells are isolated from human cord blood and samples from acute myeloid leukemia (AML) patients. Patient samples are cultured in triplicate at a density of 1×10⁶ cells/mL in MethoCult H4434 Classic Methylcellulose-Based Medium with Recombinant Cytokines for Human Cells containing MRX-2843 or vehicle. Colonies are counted after 10 days using the colony counter. Cord blood cells are incubated for 1 hour in serum-free Iscove’s modified Dulbecco’s medium (IMDM) supplemented with BIT 9500 Serum Substitute, low-density lipoproteins, and 2-ME, and then cultured in triplicate at a density of 2×10⁶ cells/mL in Methocult H4434 methylcellulose containing MRX-2843 or vehicle. Colonies are manually counted in a blinded manner after 14 days^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice are used in this study. Established leukemia cell lines or mononuclear cells isolated from samples from patients with acute myeloid leukemia (AML) (1×10⁶ to 2.5×10⁶ per mouse) are suspended in PBS and injected into the tail veins of mice to establish xenografts. All mice are 4 to 6 months of age at the time of injection and are male, with the exception of the NOMO-1, MOLM-14:D835Y, and MOLM-14:F691L NSG xenografts, which are established in female mice. Myeloblasts are detected in peripheral blood (patient-derived xenografts) or bone marrow (MOLM-14 xenografts) samples after staining with a FITC-conjugated anti-human CD45 Ab. Samples are analyzed by flow cytometry using a Gallios flow cytometer and Kaluza software. After engraftment, the mice are weighed and treated once daily with MRX-2843, quizartinib, or vehicle administered by oral gavage in a volume of 10 mL/kg. When mice appear ill or lost more than 20% of their body weight, they are euthanized^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Minson KA, et al. The MERTK/FLT3 inhibitor MRX-2843 overcomes resistance-conferring FLT3 mutations in acute myeloid leukemia. JCI Insight. 2016 Mar;1(3):e85630.

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UNC0321

发表于2024年9月30日由上海金畔生物科技有限公司

UNC0321 纯度: 99.43%

UNC0321 是一种有效的选择性组蛋白甲基转移酶 G9a 抑制剂，K_i 为 63 pM，IC₅₀ 值为 6-9 nM。UNC0321 还抑制 GLP，IC₅₀ 值为 15-23 nM。UNC0321 对 SET7/9，SET8/PreSET7，PRMT3 和 JMJD2E 无活性。

UNC0321 Chemical Structure

CAS No. : 1238673-32-9

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Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1023	In-stock
5 mg	￥902	In-stock
10 mg	￥1395	In-stock
50 mg	￥6510	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

UNC0321 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Anti-Blood Cancer Compound Library
Transcription Factor Targeted Library
Targeted Diversity Library

生物活性

UNC0321 is a potent and selective histone methyltransferase G9a inhibitor with a K_i of 63 pM and with assay-dependent IC₅₀ values of 6-9 nM. UNC0321 also inhibits GLP with assay-dependent IC₅₀ values of 15-23 nM. UNC0321 is inactive against SET7/9, SET8/PreSET7, PRMT3 and JMJD2E^[1].

IC₅₀ & Target^[1]

G9a

63 pM (Ki)

G9a

6-9 nM (IC₅₀)

GLP

15-23 nM (IC₅₀)

体外研究
(In Vitro)

In G9a ECSD and CLOT assays, the IC₅₀ values of 9 nM and 6 nM for UNC0321 (Compound 29), respectively. In GLP ECSD and CLOT assays, the IC₅₀ values of 15 nM and 23 nM for UNC0321, respectively^[1].
UNC0321 (Compound 3) reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 11 μM^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

515.69

Formula

C₂₇H₄₅N₇O₃

CAS 号

1238673-32-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 31 mg/mL (60.11 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9391 mL	9.6957 mL	19.3915 mL
5 mM	0.3878 mL	1.9391 mL	3.8783 mL
10 mM	0.1939 mL	0.9696 mL	1.9391 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (4.03 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.03 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (4.03 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.03 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.03 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.03 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Liu F, et al. Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines. J Med Chem. 2010 Aug 12;53(15):5844-57.

[2]. Liu F, et al. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J Med Chem. 2011 Sep 8;54(17):6139-50.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

UNC-2170

发表于2024年9月28日由上海金畔生物科技有限公司

UNC-2170 纯度: 99.15%

UNC-2170 是 53BP1 (IC₅₀=29 µM; K_d=22 µM) 的功能活性片段状配体。与其他九种甲基赖氨酸 (Kme) 读取器蛋白质相比，UNC-2170 对 53BP1 显示出至少17倍的选择性。53BP1 是一种 Kme 结合蛋白，在 DNA 损伤修复 (DDR) 途径中起核心作用，并被招募到双链断裂 (DSB) 位点。

UNC-2170 Chemical Structure

CAS No. : 1648707-58-7

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Free Sample (0.1-0.5 mg)		Apply now
5 mg	￥1400	In-stock
10 mg	￥2300	In-stock
25 mg	￥5000	In-stock
50 mg	￥8000	In-stock
100 mg	￥12800	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

UNC-2170 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Anti-Cancer Compound Library

生物活性

UNC-2170 is a functionally active, fragment-like ligand for 53BP1 (IC₅₀=29 µM; K_d=22 µM). UNC-2170 shows at least 17-fold selectivity for 53BP1 as compared to nine other methyl-lysine (Kme) reader proteins. 53BP1 is a Kme binding protein that plays a central role in DNA Damage Repair (DDR) pathways and is recruited to sites of double-strand breaks (DSB)^[1].

体外研究
(In Vitro)

UNC-2170 (500 µM) results in a significant increase in soluble 53BP1 as compared to untreated lysates or lysates treated with UNC2892, the negative control compound. UNC-2170 (30-100 µM; naive splenocytes cultured with LPS and IL-4 for 3.5 days) clearly phenocopies the reduction in CSR seen in 53BP1 mutant B cells^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

313.23

Formula

C₁₄H₂₁BrN₂O

CAS 号

1648707-58-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

In Vitro:

Methanol : 125 mg/mL (399.07 mM; Need ultrasonic)

DMSO : 100 mg/mL (319.25 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.1925 mL	15.9627 mL	31.9254 mL
5 mM	0.6385 mL	3.1925 mL	6.3851 mL
10 mM	0.3193 mL	1.5963 mL	3.1925 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (7.98 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.98 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (7.98 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.98 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (7.98 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.98 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。

参考文献

[1]. Perfetti MT, et al. Identification of a fragment-like small molecule ligand for the methyl-lysine binding protein, 53BP1. ACS Chem Biol. 2015;10(4):1072-1081.

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UNC0379

发表于2024年9月14日由上海金畔生物科技有限公司

UNC0379 纯度: 99.75%

UNC0379 是一个选择性的底物竞争性的赖氨酸甲基转移酶 SETD8 (KMT5A) 抑制剂，IC₅₀ 值为 7.3 μM，对其他 15 种甲基转移酶有很好的选择性。

UNC0379 Chemical Structure

CAS No. : 1620401-82-2

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1100	In-stock
5 mg	￥1000	In-stock
10 mg	￥1350	In-stock
50 mg	￥4050	In-stock
100 mg	￥5850	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

UNC0379 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Anti-Blood Cancer Compound Library
Targeted Diversity Library

生物活性

UNC0379 is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC₅₀ of 7.3 μM; selective over 15 other methyltransferases^[1].

IC₅₀ & Target

SETD8/KMT5A^[1]

分子量

413.56

Formula

C₂₃H₃₅N₅O₂

CAS 号

1620401-82-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 50 mg/mL (120.90 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4180 mL	12.0901 mL	24.1803 mL
5 mM	0.4836 mL	2.4180 mL	4.8361 mL
10 mM	0.2418 mL	1.2090 mL	2.4180 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.05 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.05 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.05 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Ma A, et al. Discovery of a Selective, Substrate-Competitive Inhibitor of the Lysine Methyltransferase SETD8. J Med Chem. 2014 Aug 14;57(15):6822-33.

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UNC0638

发表于2024年9月11日由上海金畔生物科技有限公司

UNC0638 纯度: 99.73%

UNC0638 选择性抑制 G9a 和 GLP组蛋白甲基转移酶，IC₅₀ 分别为15 nM 和 19 nM。UNC0638 具有抗 FMDV (口蹄疫病毒) 和抗 VSV (水疱性口炎病毒) 的活性。

UNC0638 Chemical Structure

CAS No. : 1255580-76-7

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥783	In-stock
5 mg	￥698	In-stock
10 mg	￥930	In-stock
50 mg	￥3255	In-stock
100 mg	￥5859	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

UNC0638 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Anti-Infection Compound Library
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Antiviral Compound Library
Autophagy Compound Library
Reprogramming Compound Library
Chemical Probe Library
Anti-Blood Cancer Compound Library

生物活性

UNC0638 selectively inhibits G9a and GLP histone methyltransferase activity with IC₅₀s of less than 15 nM and 19 nM, respectively. UNC0638 has anti-FMDV (foot-and-mouth disease virus) and anti-VSV (vesicular stomatitis virus) activities.

IC₅₀ & Target

IC50: <15 nm (g9a), 19±1 (glp)^[1]

体外研究
(In Vitro)

UNC0638, an inhibitor of G9a and GLP with excellent potency and selectivity over a wide range of epigenetic and non-epigenetic targets.The K_i of UNC0638 is determined to be 3.0±0.05 nM (n=2). Consistent with this, the Morrison K_i for UNC0638 is 3.7±0.2 nM (n=3). The selectivity of UNC0638 over a wide range of epigenetic targets is evaluated. Notably, UNC0638 is inactive against other H3K9 (SUV39H1 and SUV39H2), H3K27 (EZH2), H3K4 (SETD7, MLL and SMYD3), H3K79 (DOT1L) and H4K20 (SETD8) methyltransferases, as well as PRDM1, PRDM10 and PRDM12. In addition, UNC0638 is inactive against protein arginine methyltransferases PRMT1 and PRMT3, and HTATIP, a histone acetyltransferase. Of note, UNC0638 has weak but measurable activity against JMJD2E (IC₅₀=4,500±1,100 nM), a Jumonji protein demethylase and DNA methyltransferase DNMT1 (IC₅₀=107,000±6,000 nM). Nevertheless, the selectivity of UNC0638 for G9a and GLP over JMJD2E is >200-fold, and selectivity for G9a and GLP over DNMT1 is >5,000-fold^[1]. UNC0638 is a type of small molecule that can specifically inhibit the enzyme activity of histone methyltransferase EHMT and reduce the H3K9 dimethylation (H3K9me2) levels in cells^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

509.73

Formula

C₃₀H₄₇N₅O₂

CAS 号

1255580-76-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 30 mg/mL (58.85 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9618 mL	9.8091 mL	19.6182 mL
5 mM	0.3924 mL	1.9618 mL	3.9236 mL
10 mM	0.1962 mL	0.9809 mL	1.9618 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.90 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.90 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.90 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Vedadi M, et al. A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells. Nat Chem Biol. 2011 Jul 10;7(8):566-74.

[2]. Fu L, et al. Effects of the Histone Methyltransferase Inhibitor UNC0638 on Histone H3K9 Dimethylation of Cultured Ovine Somatic Cells and Development of Resulting Early Cloned Embryos. Reprod Domest Anim. 2014 Apr;49(2):e21-5.

[3]. Singh N, et al. Inhibition of EHMT2 Induces a Robust Antiviral Response Against Foot-and-Mouth Disease and Vesicular Stomatitis Virus Infections in Bovine Cells. J Interferon Cytokine Res. 2016 Jan;36(1):37-47.

Kinase Assay ^[1]	The enzymatic reactions are conducted in duplicate at room temperature for 1 hour in a 50 μL mixture containing PKMT assay buffer, substrate coated plate, 10 M SAM, a HMT enzyme (EZH2 (800 ng/reaction), MLL (300 ng/reaction), PRMT1 (0.5 ng/reaction), SUV39H1 (75 ng/reaction) and UNC0638 (0-1.25 μM). After enzymatic reactions, 100 μL of first antibody is added to each well and the plate is incubated at room temperature for an additional 1 h. 100 μL of secondary antibody is added to each well and the plate is incubated at room temperature for an additional 30 min. 100 μL of developer reagents are added to wells and luminescence is measured using a BioTek SynergyTM 2 microplate reader. Enzyme activity assays are performed in duplicates at each concentration. The luminescence data are analyzed using the computer software, Graphpad Prism^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	MDA-MB-231, PC3, HCT116 cells are cultured in RPMI with 10% FBS, 22RV1 cells in alphaMEM and 10% FBS, MCF7 and IMR90 cells in DMEM with 10% FBS. Cells are grown in the presence or absence of UNC0638 (10 nM, 100 nM, 1 μM, 10 μM, and 100 μM ) for stated amount of time. The media is removed and replaced with DMEM 10% FBS without phenol red supplemented with 1mg/mL of MTT and incubated for 1-2 h. Live cells reduce yellow MTT to purple formazan. The resulting formazan is solubilized in acidified isopropanol and 1% Triton and absorbance measured at 570 nm, corrected for 650 nm background^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] Standard DMPK studies in male Swiss albino mice (3 animals per data point) are conducted, following intravenous (IV, 1 mg/kg), oral (PO, 3 mg/kg), and intraperitoneal (IP, 2.5 mg/kg) administration of UNC0638. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Vedadi M, et al. A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells. Nat Chem Biol. 2011 Jul 10;7(8):566-74. [2]. Fu L, et al. Effects of the Histone Methyltransferase Inhibitor UNC0638 on Histone H3K9 Dimethylation of Cultured Ovine Somatic Cells and Development of Resulting Early Cloned Embryos. Reprod Domest Anim. 2014 Apr;49(2):e21-5. [3]. Singh N, et al. Inhibition of EHMT2 Induces a Robust Antiviral Response Against Foot-and-Mouth Disease and Vesicular Stomatitis Virus Infections in Bovine Cells. J Interferon Cytokine Res. 2016 Jan;36(1):37-47.

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UNC926 hydrochloride

发表于2024年5月28日由上海金畔生物科技有限公司

UNC926 hydrochloride

UNC926 hydrochloride 是一种 methyl-lysine (Kme) reader domain 抑制剂，可特异性抑制 L3MBTL1，其 IC₅₀ 为 3.9 μM。

UNC926 hydrochloride Chemical Structure

CAS No. : 1782573-49-2

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

UNC926 hydrochloride 的其他形式现货产品:

UNC926

生物活性	UNC926 hydrochloride is a methyl-lysine (Kme) reader domain inhibitor that inhibits L3MBTL1 with an IC₅₀ of 3.9 μM^[1].
IC₅₀ & Target	IC50: 3.9 μM (L3MBTL1), 3.2 μM (L3MBTL3), 15.6 μM (L3MBTL4)^[1]
体外研究 (In Vitro)	UNC926 also exhibits a low micromolar affinity for the close homolog, L3MBTL3 ( IC₅₀ of 3.2 μM), with a decrease in affinity for the other MBT domains and no binding to CBX7^[1]. UNC926 (1-25 μM) inhibits binding of the 3xMBT domain to H4K20me1.UNC926 inhibits the association of L3MBTL13xMBT with the appropriate histonepeptides in a dose-dependent manner. UNC926 does not have an effect on the binding of 53BP1 to H4K20me1, demonstrating specificity of UNC926 for L3MBTL1 over 53BP1^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	373.72
Formula	C₁₆H₂₂BrClN₂O
CAS 号	1782573-49-2
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Herold JM, et al. Structure-activity relationships of methyl-lysine reader antagonists. MedChemComm. 2012;3(45):45-51.

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GW284543(Synonyms: UNC10225170)

发表于2024年5月22日由上海金畔生物科技有限公司

GW284543 (Synonyms: UNC10225170) 纯度: 99.99%

GW284543 (UNC10225170) 是一个选择性的 MEK5 抑制剂。GW284543 (UNC10225170) 降低 pERK5，并下调内源性MYC 蛋白。

GW284543 Chemical Structure

CAS No. : 790186-68-4

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1210	In-stock
5 mg	￥1100	In-stock
10 mg	￥1990	In-stock
50 mg	￥6900	In-stock
100 mg	￥9900	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

GW284543 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Immunology/Inflammation Compound Library
Kinase Inhibitor Library
MAPK Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Oxygen Sensing Compound Library
Ferroptosis Compound Library
Angiogenesis Related Compound Library
Targeted Diversity Library
Anti-Liver Cancer Compound Library
Anti-Colorectal Cancer Compound Library

生物活性

GW284543 (UNC10225170) is a selective MEK5 inhibitor. GW284543 (UNC10225170) reduces pERK5, and decreases endogenous MYC protein^[1].

IC₅₀ & Target^[1]

MEK5

分子量

372.42

Formula

C₂₃H₂₀N₂O₃

CAS 号

790186-68-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 125 mg/mL (335.64 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6851 mL	13.4257 mL	26.8514 mL
5 mM	0.5370 mL	2.6851 mL	5.3703 mL
10 mM	0.2685 mL	1.3426 mL	2.6851 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (5.59 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.59 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (5.59 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.59 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (5.59 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.59 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Vaseva AV, et al. KRAS Suppression-Induced Degradation of MYC Is Antagonized by a MEK5-ERK5 Compensatory Mechanism. Cancer Cell. 2018 Nov 12;34(5):807-822.e7.

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UNC2025

发表于2024年5月20日由上海金畔生物科技有限公司

UNC2025 纯度: 99.94%

UNC2025 是一种强效、ATP 竞争性的，具有口服活性的 Mer/Flt3 抑制剂，IC₅₀ 值分别为 0.74 nM 和 0.8 nM。UNC2025 对MERTK 的选择性是 Axl 的 45 倍 (IC₅₀=122 nM; K_i=13.3 nM)。UNC2025 具有良好的 PK 特性，可用于急性白血病的研究。

UNC2025 Chemical Structure

CAS No. : 1429881-91-3

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1049	In-stock
2 mg	￥600	In-stock
5 mg	￥1000	In-stock
10 mg	￥1700	In-stock
25 mg	￥2800	In-stock
50 mg	￥4800	In-stock
100 mg	￥8000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

UNC2025 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Kinase Inhibitor Library
Protein Tyrosine Kinase Compound Library
Anti-Cancer Compound Library
CNS-Penetrant Compound Library
Orally Active Compound Library
Anti-Blood Cancer Compound Library

生物活性

UNC2025 is a potent, ATP-competitive and highly orally active Mer/Flt3 inhibitor with IC₅₀ values of 0.74 nM and 0.8 nM, respectively. UNC2025 is >45-fold selectivity for MERTK relative to Axl (IC₅₀= 122 nM; K_i = 13.3 nM). UNC2025 exhibits an excellent PK properties, and can be used for the investigation of acute leukemia^[1].

IC₅₀ & Target

IC50: 0.74 nM (Mer); 0.8 nM (Flt3)^[1]

体外研究
(In Vitro)

UNC2025 is against FLT3, MER, AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, KIT and Met with IC₅₀ values of 0.35 nM, 0.46 nM, 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM , 8.18 nM and 364 nM, respectively^[1].
UNC2025 (0-60 nM; 1 hour) mediates potent inhibition of Mer phosphorylation with an IC₅₀ of 2.7 nM in 697 B-ALL cells^[1].
UNC2025 (0-60 nM; 1 hour) results in decreased phosphorylation of Flt3 with an IC₅₀ of 14 nM in Flt3-ITD positive Molm-14 acute myeloid leukemia cells^[1].
UNC2025 (3 nM-3 μM; 1 hour) decreases p-MEK, p-AXL, p-TYRO3 expression as a concentration manner in 32D Cells^[1].
UNC2025 (14 nM–10 μM; 48 hours) inhibits MERTK signaling and colony-forming potential in a MERTK-expressing patient sample with a 20-fold difference in sensitivity of MERTK-expressing leukemia blasts relative to normal cord or marrow blood mononuclear cells^[2].
UNC2025 (25-300 nM; 1 hour) mediates potent and dose-dependent decreases in MERTK phosphorylation/activation in both cell lines and inhibition of MERTK correlated with decreased phosphorylation of previously reported MERTK-dependent signaling components STAT6, AKT, and ERK1/2^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:	32D Cells
Concentration:	0 nM, 3 nM, 10 nM, 20 nM, 30 nM, 100 nM, 1000 nM, 3000 nM
Incubation Time:	1 hour
Result:	Inhibited p-MEK, p-AXL, p-TYRO3 expression

Cell Viability Assay^[2]

Cell Line:	Mononuclear cells
Concentration:	14 nM–10μM
Incubation Time:	48 hour
Result:	Showed IC₅₀ values ranged from 9.0 nM to >10μ M with a median IC₅₀ of 2.38 μM.

Western Blot Analysis^[2]

Cell Line:	MERTK-expressing B-cell and T-cell acute lymphoid leukemia (B-ALL and T-ALL) and acute myeloid leukemia (AML) cell lines
Concentration:	25-300 nM
Incubation Time:	1 hour
Result:	Decresed p-MERTK, p-STAT6, p- AKT and p-ERK1/2 expression as a dose-dependent manner.

体内研究
(In Vivo)

UNC2025 (intravenous injection or oral adminstration; 3 mg/kg) exhibits an excellent PK properties: low clearance (9.2 mL/min kg), longer half-life (3.8 h), and high oral exposure (100%), it shows T_max, C_max, and AUClast 0.50 hour, 1.6 μM, and 9.2 h μM, respectively^[2].
UNC2025 (orally adminstration; 50 or 75 mg/kg; 34 and 70 days) mediates a statistically significant dose-dependent reduction in tumor burden relative to vehicle. mediates dose-dependent increases in median survival from 26 days after initiation of treatment in vehicle-treated mice, to 34 and 70 days in mice treated with 50 or 75 mg/kg UNC2025, respectively^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	NSG mice injected with 697 B-ALL cells^[2]
Dosage:	50 or 75 mg/kg
Administration:	Orally adminstration
Result:	Delayed the disease progression.

分子量

476.66

Formula

C₂₈H₄₀N₆O

CAS 号

1429881-91-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 33.33 mg/mL (69.92 mM; Need ultrasonic and warming)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0979 mL	10.4897 mL	20.9793 mL
5 mM	0.4196 mL	2.0979 mL	4.1959 mL
10 mM	0.2098 mL	1.0490 mL	2.0979 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.24 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.24 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Zhang W, et al. UNC2025, a Potent and Orally Bioavailable MER/FLT3 Dual Inhibitor. J Med Chem. 2014 Aug 28;57(16):7031-41.

[2]. DeRyckere D, et al. UNC2025, a MERTK Small-Molecule Inhibitor, Is Therapeutically Effective Alone and in Combination with CL14377 in Leukemia Models.Clin Cancer Res. 2017 Mar 15;23(6):1481-1492.

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UNC6934

发表于2024年5月7日由上海金畔生物科技有限公司

UNC6934 纯度: 98.51%

UNC6934 是一种靶向 NSD2 的 PWWP 结构域的化学探针，可定位核仁。

UNC6934 Chemical Structure

CAS No. : 2561494-77-5

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥38500	In-stock
5 mg	￥3500	In-stock
10 mg	￥5500	In-stock
25 mg	￥11000	In-stock
50 mg		询价
100 mg		询价

* Please select Quantity before adding items.

UNC6934 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Anti-Blood Cancer Compound Library

生物活性

UNC6934, a chemical probe targeting the PWWP domain, alters NSD2 nucleolar localization.

分子量

443.45

Formula

C₂₄H₂₁N₅O₄

CAS 号

2561494-77-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 25 mg/mL (56.38 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2550 mL	11.2752 mL	22.5505 mL
5 mM	0.4510 mL	2.2550 mL	4.5101 mL
10 mM	0.2255 mL	1.1275 mL	2.2550 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (5.64 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.64 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.64 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.64 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.64 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.64 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。

参考文献

[1]. Dilworth D, et al. A chemical probe targeting the PWWP domain alters NSD2 nucleolar localization. Nat Chem Biol. 2022 Jan;18(1):56-63.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

UNC0224

发表于2024年4月28日由上海金畔生物科技有限公司

UNC0224 纯度: 99.31%

UNC0224 是一种有效的选择性的组蛋白甲基转移酶 G9a 抑制剂，K_i 为 2.6 nM，IC₅₀ 值为 15 nM，K_d 为 23 nM。UNC0224 还有效抑制 GLP，IC₅₀ 值为 20-58 nM。UNC0224 对 SET7/9，SET8/PreSET7，PRMT3 和 JMJD2E 无活性。

UNC0224 Chemical Structure

CAS No. : 1197196-48-7

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥992	In-stock
5 mg	￥902	In-stock
10 mg	￥1395	In-stock
50 mg	￥6510	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

UNC0224 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Anti-Blood Cancer Compound Library
Transcription Factor Targeted Library
Targeted Diversity Library

生物活性

UNC0224 is a potent and selective histone methyltransferase G9a inhibitor with a K_i of 2.6 nM, an IC₅₀ of 15 nM and a K_d of 23 nM. UNC0224 also potently inhibits b>GLP with assay-dependent IC₅₀ values of 20-58 nM. UNC0224 is inactive against SET7/9, SET8/PreSET7, PRMT3 and JMJD2E^[1]^[2].

IC₅₀ & Target^[1]^[2]

G9a

15 nM (IC₅₀)

G9a

2.6 nM (Ki)

G9a

23 nM (Kd)

GLP

20-58 nM (IC₅₀)

体外研究
(In Vitro)

In G9a ECSD and CLOT assays, the IC₅₀ values of 43 nM and 57 nM for UNC0224 (Compound 10), respectively. In GLP ECSD and CLOT assays, the IC₅₀ values of 50 nM and 58 nM for UNC0224, respectively. In ITC experiments, the K_d value of UNC0224 to the G9a protein is 23 nM^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

485.67

Formula

C₂₆H₄₃N₇O₂

CAS 号

1197196-48-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 16.67 mg/mL (34.32 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0590 mL	10.2951 mL	20.5901 mL
5 mM	0.4118 mL	2.0590 mL	4.1180 mL
10 mM	0.2059 mL	1.0295 mL	2.0590 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 1.67 mg/mL (3.44 mM); Clear solution

此方案可获得 ≥ 1.67 mg/mL (3.44 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 1.67 mg/mL (3.44 mM); Clear solution

此方案可获得 ≥ 1.67 mg/mL (3.44 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 1.67 mg/mL (3.44 mM); Clear solution

此方案可获得 ≥ 1.67 mg/mL (3.44 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Liu F, et al. Discovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a. J Med Chem. 2009 Dec 24;52(24):7950-3.

[2]. Liu F, et al. Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines. J Med Chem. 2010 Aug 12;53(15):5844-57.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

生物活性分子抑制剂UNC6852

发表于2024年4月6日由上海金畔生物科技有限公司

生物活性分子抑制剂特异性抑制剂激动剂化合物库重组蛋白 UNC6852 纯度: 98.68%

UNC6852是一种基于 PROTAC 技术的，选择性的 PRC2 降解剂，包含了一个 EED 配体和一个 von Hippel-Lindau 配体，对 EED 作用的 IC₅₀ 值为 247 nM。

UNC6852 Chemical Structure

CAS No. : 2688842-08-0

规格	价格	是否有货
5 mg	￥3000	询价
10 mg	￥5200	In-stock
25 mg	￥9800	In-stock
50 mg	￥15000	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

UNC6852 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Anti-Blood Cancer Compound Library

生物活性

UNC6852 is a selective polycomb repressive complex 2 (PRC2) degrader based on PROTAC and contains an EED (embryonic ectoderm development) ligand and a von Hippel-Lindau ligand, with an IC₅₀ of 247 nM for EED^[1].

IC₅₀ & Target

IC50: 247 nM (EED)^[1]

体外研究
(In Vitro)

UNC6852 mediates PRC2 degradation^[1].
UNC6852 displays no cellular toxicity at concentrations up to 30 μM for HeLa Cells^[1].
UNC6852 (10 μM; 1-72 hours) results in a decrease in the levels of both EED and EZH2^[1].
UNC6852 facilitates PRC2 degradation via VHL recruitment^[1].
UNC6852 selectively degrades EED and EZH2^[1].
UNC6852 reduces H3K27me3 levels and DLBCL cell proliferation^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:	DLBCL Cells
Concentration:	3 μM
Incubation Time:	0 -10 days
Result:	Exhibited anti-proliferative effects.

Western Blot Analysis^[1]

Cell Line:	HeLa Cells
Concentration:	10 μM
Incubation Time:	1 hours, 4 hours, 8 hours, 10 hours, 16 hours, 20 hours, 24 hours, 48 hours, 72 hours
Result:	Resulted in a decrease in the levels of both EED and EZH2.

分子量

832.97

Formula

C₄₃H₄₈N₁₀O₆S

CAS 号

2688842-08-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL (120.05 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.2005 mL	6.0026 mL	12.0052 mL
5 mM	0.2401 mL	1.2005 mL	2.4010 mL
10 mM	0.1201 mL	0.6003 mL	1.2005 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 5 mg/mL (6.00 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (6.00 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 5 mg/mL (6.00 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (6.00 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 5 mg/mL (6.00 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (6.00 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Potjewyd F, et al. Degradation of Polycomb Repressive Complex 2 with an EED-Targeted Bivalent Chemical Degrader. Cell Chem Biol. 2020 Jan 16;27(1):47-56.e15.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

UNC0646

发表于2024年3月20日由上海金畔生物科技有限公司

UNC0646 纯度: 99.82%

UNC0646 是一种有效的选择性组蛋白甲基转移酶 G9a 抑制剂，其 IC₅₀ 为 6 nM。UNC0646 还是一种有效的 GLP 抑制剂 (IC₅₀ <15 nm)，对 G9a/GLP 的选择性比 SETD7，SUV39H2，SETD8 和 PRMT3 高。UNC0646 降低 MDA-MB-231 细胞中 H3K9me2 的水平，IC₅₀ 为 26 nM。

UNC0646 Chemical Structure

CAS No. : 1320288-17-2

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1018	In-stock
5 mg	￥744	In-stock
10 mg	￥1050	In-stock
50 mg	￥3510	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

UNC0646 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Anti-Blood Cancer Compound Library
Transcription Factor Targeted Library
Targeted Diversity Library

生物活性

UNC0646 is a potent and selective histone methyltransferase G9a inhibitor with an IC₅₀ of 6 nM. UNC0646 is also a potent GLP inhibitor (IC₅₀ <15 nm) and highly selective for G9a/GLP over SETD7, SUV39H2, SETD8 and PRMT3. UNC0646 reduces H3K9me2 levels in MDA-MB-231 cells with an IC₅₀ of 26 nM^[1].

IC₅₀ & Target

G9a

6 nM (IC₅₀)

GLP

<15 nM (IC₅₀)

体外研究
(In Vitro)

UNC0646 (Compound 6) has high cellular potency and excellent separation of functional potency versus cell toxicity in a variety of cell lines. UNC0646 is highly potent in reducing H3K9me2 levels and has low cell toxicity. UNC0646 reduces H3K9me2 levels with ICW IC₅₀ values of 26 nM, 10 nM, 12 nM, 14 nM, 68 nM, 86 nM and 10 nM in MDA-MB-231, MCF7, PC3, 22RV1, HCT116 wt, HCT 116 p53^-/- and IMR90 cell lines, respectively^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

621.90

Formula

C₃₆H₅₉N₇O₂

CAS 号

1320288-17-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 50 mg/mL (80.40 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 80°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6080 mL	8.0399 mL	16.0798 mL
5 mM	0.3216 mL	1.6080 mL	3.2160 mL
10 mM	0.1608 mL	0.8040 mL	1.6080 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 4.55 mg/mL (7.32 mM); Clear solution

此方案可获得 ≥ 4.55 mg/mL (7.32 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 45.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (4.02 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.02 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.02 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.02 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。

参考文献

[1]. Liu F, et al. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J Med Chem. 2011 Sep 8;54(17):6139-50.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

UNC0646

发表于2024年3月20日由上海金畔生物科技有限公司

UNC0646 纯度: 99.82%

UNC0646 Chemical Structure

CAS No. : 1320288-17-2

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1018	In-stock
5 mg	￥744	In-stock
10 mg	￥1050	In-stock
50 mg	￥3510	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

UNC0646 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Anti-Blood Cancer Compound Library
Transcription Factor Targeted Library
Targeted Diversity Library

生物活性

IC₅₀ & Target

G9a

6 nM (IC₅₀)

GLP

<15 nM (IC₅₀)

体外研究
(In Vitro)

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

621.90

Formula

C₃₆H₅₉N₇O₂

CAS 号

1320288-17-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 50 mg/mL (80.40 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 80°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6080 mL	8.0399 mL	16.0798 mL
5 mM	0.3216 mL	1.6080 mL	3.2160 mL
10 mM	0.1608 mL	0.8040 mL	1.6080 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 4.55 mg/mL (7.32 mM); Clear solution

此方案可获得 ≥ 4.55 mg/mL (7.32 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 45.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (4.02 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.02 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.02 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.02 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。

参考文献

[1]. Liu F, et al. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J Med Chem. 2011 Sep 8;54(17):6139-50.

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