Vacquinol-1(Synonyms: NSC13316)

发表于2024年11月18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。

Vacquinol-1 (Synonyms: NSC13316)

Vacquinol-1 (NSC13316) 是一种 MKK4 特异性激活剂，可激活 MAPK 通路。 Vacquinol-1 在多形性胶质母细胞瘤 (GBM) 小鼠模型中特异性诱导人胶质母细胞瘤细胞 (GC) 死亡、减缓肿瘤进展并延长生存期。 Vacquinol-1 还诱导肝细胞癌 (HCC) 细胞凋亡。

Vacquinol-1 Chemical Structure

CAS No. : 5428-80-8

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生物活性

Vacquinol-1 (NSC13316) is a MKK4-specific activator that activates MAPK pathways^[1]. Vacquinol-1 specifically induces human glioblastoma cell (GC) death, attenuates tumor progression and prolongs survival in a glioblastoma multiforme (GBM) mouse model^[2]. Vacquinol-1 also induces apoptosis in hepatocellular carcinoma (HCC)cell^[3].

分子量

352.86

Formula

C₂₁H₂₁ClN₂O

CAS 号

5428-80-8

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.

溶解性数据

In Vitro:

DMSO : 30 mg/mL (85.02 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	2.8340 mL	14.1699 mL	28.3399 mL
5 mM	0.5668 mL	2.8340 mL	5.6680 mL
10 mM	0.2834 mL	1.4170 mL	2.8340 mL

参考文献

[1]. Sun SL, Li X, Su N, et al. Vacquinol‑1 induces apoptosis in hepatocellular carcinoma cell. Mol Med Rep. 2018;18(1):557-563.

[2]. Sander P, Mostafa H, Soboh A, et al. Vacquinol-1 inducible cell death in glioblastoma multiforme is counter regulated by TRPM7 activity induced by exogenous ATP. Oncotarget. 2017;8(21):35124-35137.

[3]. Chao Wu, et al. Salvianolic acid B exerts anti-liver fibrosis effects via inhibition of MAPK-mediated phospho-Smad2/3 at linker regions in vivo and in vitro. Life Sci. 2019 Dec 15;239:116881.

[4]. Yufeng Shi, et al. The soft underbelly of tumor cells. Cell Res. 2014 Aug;24(8):910-1.

[5]. Shu-Lan Sun, et al. Vacquinol 1 induces apoptosis in hepatocellular carcinoma cell. Mol Med Rep. 2018 Jul;18(1):557-563.

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Vacquinol-1(Synonyms: NSC13316)

发表于2024年11月18日由上海金畔生物科技有限公司

Vacquinol-1 (Synonyms: NSC13316)

Vacquinol-1 Chemical Structure

CAS No. : 5428-80-8

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

* Please select Quantity before adding items.

生物活性

分子量

352.86

Formula

C₂₁H₂₁ClN₂O

CAS 号

5428-80-8

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.

溶解性数据

In Vitro:

DMSO : 30 mg/mL (85.02 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	2.8340 mL	14.1699 mL	28.3399 mL
5 mM	0.5668 mL	2.8340 mL	5.6680 mL
10 mM	0.2834 mL	1.4170 mL	2.8340 mL

参考文献

[1]. Sun SL, Li X, Su N, et al. Vacquinol‑1 induces apoptosis in hepatocellular carcinoma cell. Mol Med Rep. 2018;18(1):557-563.

[2]. Sander P, Mostafa H, Soboh A, et al. Vacquinol-1 inducible cell death in glioblastoma multiforme is counter regulated by TRPM7 activity induced by exogenous ATP. Oncotarget. 2017;8(21):35124-35137.

[3]. Chao Wu, et al. Salvianolic acid B exerts anti-liver fibrosis effects via inhibition of MAPK-mediated phospho-Smad2/3 at linker regions in vivo and in vitro. Life Sci. 2019 Dec 15;239:116881.

[4]. Yufeng Shi, et al. The soft underbelly of tumor cells. Cell Res. 2014 Aug;24(8):910-1.

[5]. Shu-Lan Sun, et al. Vacquinol 1 induces apoptosis in hepatocellular carcinoma cell. Mol Med Rep. 2018 Jul;18(1):557-563.

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Vacquinol-1(Synonyms: NSC13316)

发表于2024年11月18日由上海金畔生物科技有限公司

Vacquinol-1 (Synonyms: NSC13316)

Vacquinol-1 Chemical Structure

CAS No. : 5428-80-8

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

* Please select Quantity before adding items.

生物活性

分子量

352.86

Formula

C₂₁H₂₁ClN₂O

CAS 号

5428-80-8

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.

溶解性数据

In Vitro:

DMSO : 30 mg/mL (85.02 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	2.8340 mL	14.1699 mL	28.3399 mL
5 mM	0.5668 mL	2.8340 mL	5.6680 mL
10 mM	0.2834 mL	1.4170 mL	2.8340 mL

参考文献

[1]. Sun SL, Li X, Su N, et al. Vacquinol‑1 induces apoptosis in hepatocellular carcinoma cell. Mol Med Rep. 2018;18(1):557-563.

[2]. Sander P, Mostafa H, Soboh A, et al. Vacquinol-1 inducible cell death in glioblastoma multiforme is counter regulated by TRPM7 activity induced by exogenous ATP. Oncotarget. 2017;8(21):35124-35137.

[3]. Chao Wu, et al. Salvianolic acid B exerts anti-liver fibrosis effects via inhibition of MAPK-mediated phospho-Smad2/3 at linker regions in vivo and in vitro. Life Sci. 2019 Dec 15;239:116881.

[4]. Yufeng Shi, et al. The soft underbelly of tumor cells. Cell Res. 2014 Aug;24(8):910-1.

[5]. Shu-Lan Sun, et al. Vacquinol 1 induces apoptosis in hepatocellular carcinoma cell. Mol Med Rep. 2018 Jul;18(1):557-563.

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BRD7389

发表于2024年10月19日由上海金畔生物科技有限公司

BRD7389

BRD7389 是一种特异性的 RSK 家族激酶抑制剂，对 RSK1，RSK2 和 RSK3 的 IC₅₀ 分别为 1.5 μM，2.4 μM 和 1.2 μM。BRD7389 可以诱导胰腺 α 细胞中胰岛素表达。

BRD7389 Chemical Structure

CAS No. : 376382-11-5

规格	价格	是否有货
10 mg	￥7200	询问价格 & 货期

* Please select Quantity before adding items.

生物活性

BRD7389 is a specific RSK family kinase inhibitor with IC₅₀s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively. BRD7389 is a small-molecule inducer of insulin expression in pancreatic α-cells^[1].

IC₅₀ & Target^[1]

RSK1

1.5 μM (IC₅₀)

RSK2

2.4 μM (IC₅₀)

RSK3

1.2 μM (IC₅₀)

CDK5/p35

6.5 μM (IC₅₀)

DRAK1

2.8 μM (IC₅₀)

FLT3

3.5 μM (IC₅₀)

PIM1

3.7 μM (IC₅₀)

PKG1α

6.5 μM (IC₅₀)

SGK

13.8 μM (IC₅₀)

体外研究
(In Vitro)

BRD7389 (0.425-6.8 μM) induces insulin expression in mouse α-cells after 3 days treatment. BRD7389 induces a dose-dependent up-regulation of insulin (Ins2) mRNA, peaking at 0.85 μM; 5 days treatment with BRD7389 results in greater induction of insulin gene expression, about 50-fold at 0.85 μM^[1].
BRD7389 (0.85-6.8μM) significantly up-regulates Pdx1 mRNA expression in mouse α-cell line^[1].
BRD7389 also increases β-cell-specific gene expression in primary human islet cells^[1].
BRD7389 (1 μM; added 30 min prior to Carbachol treatment 48 h) fully abolishes carbachols timulated cell proliferation, but has little effect on the basal level of proliferation^[2].

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

RT-PCR^[1]

Cell Line:	Mouse α-cell line
Concentration:	0.425, 0.85, 1.7, 3.4, 6.8 μM
Incubation Time:	3 days and 5 days
Result:	Up-regulated expression of Pdx1.

Cell Proliferation Assay^[2]

Cell Line:	SNU-407 colon cancer cell
Concentration:	1 μM
Incubation Time:	Added 30 min prior to Carbachol treatment (48 h)
Result:	Almost completely blocked Carbachol (1 mM)-stimulated cell proliferation.

分子量

366.41

Formula

C₂₄H₁₈N₂O₂

CAS 号

376382-11-5

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)

参考文献

[1]. Fomina-Yadlin D, et al. Small-molecule inducers of insulin expression in pancreatic alpha-cells. Proc Natl Acad Sci U S A. 2010 Aug 24;107(34):15099-104.

[2]. Park YS, et al. EGFR and PKC are involved in the activation of ERK1/2 and p90 RSK and the subsequent proliferation of SNU-407 colon cancer cells by muscarinic acetylcholine receptors. Mol Cell Biochem. 2012 Nov;370(1-2):191-8.

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Spautin-1

发表于2024年10月14日由上海金畔生物科技有限公司

Spautin-1 纯度: 99.26%

Spautin-1是一种特异性和有效的自噬抑制剂，可抑制泛素特异性肽酶USP10和 USP13，IC₅₀s 约为0.6-0.7 μM。

Spautin-1 Chemical Structure

CAS No. : 1262888-28-7

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥610	In-stock
5 mg	￥550	In-stock
10 mg	￥700	In-stock
50 mg	￥2500	In-stock
100 mg	￥4500	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

Spautin-1 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Apoptosis Compound Library
Anti-Cancer Compound Library
Autophagy Compound Library

生物活性

Spautin-1 is a specific and potent autophagy inhibitor which inhibits ubiquitin-specific peptidases, USP10 and USP13 with IC₅₀s of 0.6-0.7 μM.

体外研究
(In Vitro)

Spautin-1 enhances imatinib mesylate (IM)-induced CmL cell apoptosis by reducing the expression of the anti-apoptotic proteins Mcl-1 and Bcl-2. The pro-apoptotic activity of spautin-1 is associated with activation of GSK3β, an important downstream effector of PI3K/AKT. Spautin-1 enhances IM-induced cytotoxicity in CmL cell line K562, decreasing the IC₅₀ from 1 to 0.5 μM^[1]. The mechanism of spautin-1 acting on acute pancreatitis is associated with impaired autophagy inhibition^[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.

体内研究
(In Vivo)

Spautin-1 ameliorates the pathogenesis of acute pancreatitis induced by cerulein or L-arginine. Spautin-1 pretreatment significantly diminishes the elevation of serum amylase and lipase levels, which are indicative of trypsin activity. Increasing levels of serum TNFα caused by cerulein are inhibited in the presence of spautin-1. Spautin-1 treatment can ameliorate the inflammation damage induced by cerulein, such as edema, degeneration, coagulative necrosis and infiltration of inflammatory 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

271.26

Formula

C₁₅H₁₁F₂N₃

CAS 号

1262888-28-7

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 : 50 mg/mL (184.33 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.6865 mL	18.4325 mL	36.8650 mL
5 mM	0.7373 mL	3.6865 mL	7.3730 mL
10 mM	0.3687 mL	1.8433 mL	3.6865 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：

——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 (9.22 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (9.22 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 (9.22 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (9.22 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]. Shao S, et al. Spautin-1, a novel autophagy inhibitor, enhances imatinib-induced apoptosis in chronic myeloid leukemia. Int J Oncol. 2014 May;44(5):1661-1668.

[2]. Xiao J, et al. Spautin-1 Ameliorates Acute Pancreatitis via Inhibiting Impaired Autophagy and Alleviating Calcium Overload. Mol Med. 2016 Aug 18;22.

Cell Assay ^[1]	Spautin-1 is dissolved in DMSO. Cell proliferation is evaluated using CCK-8 kit. K562 cells (1×10⁵/mL) are seeded into 96-well plates in triplicate and then treated with 125 to 4,000 nM IM alone or in combi¬nation with spautin-1 (10 μM). After 48 h of incubation, 10 μL of CCK-8 reagent is added to each well. Four hours later, the absorbance is read at 450 nm using a 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.
Animal Administration ^[2]	Mice: In this study, mice models with acute pancreatitis, including cerulein- and L-arginine-induced models, are constructed. For the cerulein-induced model, four intraperitoneal injections of cerulein (50 μg/kg body weight) are given consecutively at hourly intervals; The L-arginine-induced model received hourly intraperitoneal injections of 1.4 g/kg (optimal dosage for this study) L-arginine three times^[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.
参考文献	[1]. Shao S, et al. Spautin-1, a novel autophagy inhibitor, enhances imatinib-induced apoptosis in chronic myeloid leukemia. Int J Oncol. 2014 May;44(5):1661-1668. [2]. Xiao J, et al. Spautin-1 Ameliorates Acute Pancreatitis via Inhibiting Impaired Autophagy and Alleviating Calcium Overload. Mol Med. 2016 Aug 18;22.

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6RK73

发表于2024年7月28日由上海金畔生物科技有限公司

6RK73 纯度: 99.41%

6RK73 是一种共价不可逆的特异性 UCHL1 抑制剂，IC₅₀ 为 0.23 µM。6RK73 对 UCHL3 几乎没有抑制效果 (IC₅₀=236 µM)。6RK73 特异性抑制乳腺癌中 UCHL1 的活性。

6RK73 Chemical Structure

CAS No. : 1895050-66-4

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥4180	In-stock
5 mg	￥3800	In-stock
10 mg	￥6500	In-stock
50 mg	￥18000	In-stock
100 mg	￥28000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

6RK73 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Cell Cycle/DNA Damage Compound Library
Anti-Cancer Compound Library
Anti-Aging Compound Library
Ubiquitination Compound Library
Anti-Breast Cancer Compound Library

生物活性

6RK73 is a covalent irreversible and specific UCHL1 inhibitor with an IC₅₀ of 0.23 µM. 6RK73 shows almost no inhibition of UCHL3 (IC₅₀=236 µM). 6RK73 specifically inhibit UCHL1 activity in breast cancer^[1].

IC₅₀ & Target

IC50: 0.23 µM (UCHL1), 236 µM (UCHL3)^[1]

体外研究
(In Vitro)

6RK73 (5 µM; 1-3 hours) treatment displays strong inhibition of the TGFβ-induced pSMAD2 and pSMAD3, and a decrease of TβRI and total SMAD protein levels in MDA-MB-436 cells^[1].
6RK73(5 µM; 24-48 hours) results migration significantly slower than the DMSO control group in MDA-MB-436 cells^[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 Viability Assay^[1]

Cell Line:	MDA-MB-436 cells
Concentration:	5 µM
Incubation Time:	24, 48 hours
Result:	Migrated significantly slower than the DMSO control group

Western Blot Analysis^[1]

Cell Line:	MDA-MB-436 cells
Concentration:	5 µM
Incubation Time:	1, 2, 3 hours
Result:	Displayed strong inhibition of the TGFβ-induced pSMAD2 and pSMAD3, and a decrease of TβRI and total SMAD protein levels.

体内研究
(In Vivo)

6RK73 displays a potent inhibition of breast cancer extravasation in zebrafish^[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

307.37

Formula

C₁₃H₁₇N₅O₂S

CAS 号

1895050-66-4

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 (406.68 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.2534 mL	16.2670 mL	32.5341 mL
5 mM	0.6507 mL	3.2534 mL	6.5068 mL
10 mM	0.3253 mL	1.6267 mL	3.2534 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 (6.77 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.77 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 (6.77 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.77 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 (6.77 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.77 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 S, et al. Deubiquitinase activity profiling identifies UCHL1 as a candidate oncoprotein that promotes TGFβ-induced breast cancer metastasis. Clin Cancer Res. 2019 Dec 19. pii: clincanres.1373.2019.

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D609

发表于2024年7月16日由上海金畔生物科技有限公司

D609 纯度: ≥98.0%

D609 是一种选择性的磷脂酰胆碱特异性的磷脂酶C (phosphatidyl choline-specific phospholipase C) 抑制剂，K_i 值为 6.4 μM。

D609 Chemical Structure

CAS No. : 83373-60-8

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥550	In-stock
5 mg	￥500	In-stock
10 mg	￥800	In-stock
50 mg	￥2800	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

D609 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Metabolism/Protease Compound Library
Anti-Cancer Compound Library
Lipid Metabolism Compound Library
Targeted Diversity Library

生物活性

D609 is a selective competitive inhibitor of phosphatidyl choline-specific phospholipase C (PC-PLC), with K_i of 6.4 μM.

IC₅₀ & Target

Ki: 6.4 μM (PC-PLC)

分子量

266.46

Formula

C₁₁H₁₅KOS₂

CAS 号

83373-60-8

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 (375.29 mM; Need ultrasonic)

H₂O : 2 mg/mL (7.51 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.7529 mL	18.7645 mL	37.5291 mL
5 mM	0.7506 mL	3.7529 mL	7.5058 mL
10 mM	0.3753 mL	1.8765 mL	3.7529 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: ≥ 3 mg/mL (11.26 mM); Clear solution

此方案可获得 ≥ 3 mg/mL (11.26 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 30.0 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: ≥ 3 mg/mL (11.26 mM); Clear solution

此方案可获得 ≥ 3 mg/mL (11.26 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 30.0 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: ≥ 3 mg/mL (11.26 mM); Clear solution

此方案可获得 ≥ 3 mg/mL (11.26 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 30.0 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]. Kalluri HS, et al. D609 inhibits the proliferation of neural progenitor cells.Neuroreport. 2010 Jul 14;21(10):700-3.

[2]. Milhas D, et al. The Tricyclodecan-9-yl-xanthogenate D609 Triggers Ceramide Increase and Enhances FasL-Induced Caspase-Dependent and -Independent Cell Death in T Lymphocytes.Int J Mol Sci. 2012;13(7):8834-52. Epub 2012 Jul 16.

[3]. Gusain A, et al. Anti-proliferative effects of tricyclodecan-9-yl-xanthogenate (D609) involve ceramide and cell cycle inhibition.Mol Neurobiol. 2012 Jun;45(3):455-64. Epub 2012 Mar 14.

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BCI(Synonyms: (E)-BCI)

发表于2024年7月14日由上海金畔生物科技有限公司

BCI (Synonyms: (E)-BCI) 纯度: 99.83%

BCI 是一种双重特异性磷酸酶 (DUSP) 的变构抑制剂。BCI 特异性抑制 DUSP6 和 DUSP1 的 EC₅₀ 分别为 13.3 和 8.0 μM。BCI 不抑制 DUSP5。

BCI Chemical Structure

CAS No. : 1245792-51-1

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1050	In-stock
1 mg	￥600	In-stock
5 mg	￥1500	In-stock
10 mg	￥2500	In-stock
100 mg	￥12750	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

BCI 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Immunology/Inflammation Compound Library
Metabolism/Protease Compound Library
Anti-Cancer Compound Library
Phosphatase Inhibitor Library

生物活性

BCI is an allosteric inhibitor of dual specificity phosphatase (DUSP). BCI specifically inhibits DUSP6 and DUSP1 with EC₅₀s of 13.3 and 8.0 μM in cells, respectively. BCI does not inhibit DUSP5^[1].

分子量

317.42

Formula

C₂₂H₂₃NO

CAS 号

1245792-51-1

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 (393.80 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.1504 mL	15.7520 mL	31.5040 mL
5 mM	0.6301 mL	3.1504 mL	6.3008 mL
10 mM	0.3150 mL	1.5752 mL	3.1504 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 (6.55 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (6.55 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 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% corn oil

Solubility: ≥ 2.08 mg/mL (6.55 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.55 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]. Korotchenko VN, et al. In vivo structure-activity relationship studies support allosteric targeting of a dual specificity phosphatase. Chembiochem. 2014 Jul 7;15(10):1436-45.

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ON1231320

发表于2024年7月5日由上海金畔生物科技有限公司

ON1231320 纯度: 99.24%

ON1231320 是一种高度特异性的 polo 样激酶 2 (PLK2) 抑制剂，IC₅₀ 为 0.31 µM。ON1231320 在有丝分裂 G2/M 期阻断肿瘤细胞周期进程，导致细胞凋亡。ON1231320 是一种芳基磺酰基吡啶并嘧啶酮，具有抗肿瘤活性。

ON1231320 Chemical Structure

CAS No. : 1312471-39-8

规格	价格	是否有货
5 mg	￥1000	In-stock
10 mg	￥1700	In-stock
25 mg	￥3500	In-stock
50 mg	￥5500	In-stock
100 mg	￥9500	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

ON1231320 相关产品

•相关化合物库:

Bioactive Compound Library Plus

生物活性

ON1231320 is a highly specific polo like kinase 2 (PLK2) inhibitor with an IC₅₀ of 0.31 µM. ON1231320 blocks tumor cell cycle progression in the G2/M phase in mitosis, causing apoptotic cell death. ON1231320, an arylsulfonyl pyrido-pyrimidinone, has antitumor activity^[1]^[2].

IC₅₀ & Target^[1]

PLK2

0.31 μM (IC₅₀)

PLK1

>10 μM (IC₅₀)

PLK3

>10 μM (IC₅₀)

PLK4

>10 μM (IC₅₀)

体外研究
(In Vitro)

ON1231320 (Compound 7ao) has no inhibitory activity against PLK1, PLK3 and PLK4 (all IC₅₀>10 µM)^[1].
ON1231320 (0-5 µM; 24 hours) activates programmed cell death in human tumor cells^[1].
ON1231320 inhibits cell proliferation in 16 tumor cell lines (DU145, MCF-7, BT474, SK-OV-3, MIA-PaCa-2, SK-MEL-28, A549, U87, COLO-205, HELA, H1975, RAJI, U205, K562, GRANTA-519; IC₅₀= 0.035-0.2 µM)^[1].
ON1231320 does not appreciably inhibit tubulin polymerization^[1]. ON1231320 does not affect normal human fibroblasts^[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.

Apoptosis Analysis^[1]

Cell Line:	U2OS cells
Concentration:	0-5 µM
Incubation Time:	24 hours
Result:	Increased the activity of Caspases 3/7 in a dose-dependent manner. Induced apoptosis.

体内研究
(In Vivo)

ON1231320 (Compound 7ao; 75 mg/kg; IP; alternate days (Q2D) for 20 days) results in significant inhibition of tumor growth^[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 Model:	6-8 week old NCR nu/nu female mice with MDAMB-231 triple negative breast cancer cells^[1]
Dosage:	75 mg/kg
Administration:	IP; alternate days (Q2D) for 20 days
Result:	Resulted in significant inhibition of tumor growth (86.5%)

分子量

467.45

Formula

C₂₂H₁₅F₂N₅O₃S

CAS 号

1312471-39-8

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 : 25 mg/mL (53.48 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1393 mL	10.6963 mL	21.3927 mL
5 mM	0.4279 mL	2.1393 mL	4.2785 mL
10 mM	0.2139 mL	1.0696 mL	2.1393 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% (20% SBE-β-CD in saline)

Solubility: 2.5 mg/mL (5.35 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (5.35 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 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

*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]. M V Ramana Reddy, et al. Discovery of 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (7ao) as a potent selective inhibitor of Polo like kinase 2 (PLK2). Bioorg Med Chem. 2016 Feb 15;24(4):521-44.

[2]. Shashidhar S. Jatiani, et al. Abstract 643: Targeting cancer with a selective ATP-mimetic inhibitor of polo like kinase-2.

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DUB-IN-1

发表于2024年7月5日由上海金畔生物科技有限公司

DUB-IN-1 纯度: 99.59%

DUB-IN-1 是一种有活性的泛素特异性蛋白酶 (ubiquitin-specific proteases) 抑制剂，对 USP8 的 IC₅₀ 值为 0.85 μM。

DUB-IN-1 Chemical Structure

CAS No. : 924296-18-4

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥3080	In-stock
5 mg	￥2800	In-stock
10 mg	￥4500	In-stock
50 mg	￥13500	In-stock
100 mg	￥21600	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

DUB-IN-1 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Cell Cycle/DNA Damage Compound Library
Anti-Cancer Compound Library
Anti-Aging Compound Library
Ubiquitination Compound Library

生物活性

DUB-IN-1 is an active inhibitor of ubiquitin-specific proteases (USPs), with an IC₅₀ of 0.85 μM for USP8^[1].

IC₅₀ & Target

IC50: 0.24 μM (USP8)^[1]

体外研究
(In Vitro)

DUBs-IN-1 (22 d) is an active inhibitor of ubiquitin-specific proteases, with an IC₅₀ of 0.85 μM for USP8. DUBs-IN-1 is inactive toward USP7 (IC₅₀, >100 μM). DUBs-IN-1 and its analogs reduce the viability of HCT116 colon and PC-3 prostate cancer cell lines with IC₅₀s ranging from 0.5 μM to 1.5 μM^[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

337.33

Formula

C₂₀H₁₁N₅O

CAS 号

924296-18-4

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 : 100 mg/mL (296.45 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.9645 mL	14.8223 mL	29.6446 mL
5 mM	0.5929 mL	2.9645 mL	5.9289 mL
10 mM	0.2964 mL	1.4822 mL	2.9645 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 (7.41 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (7.41 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 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 (7.41 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.41 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]. Colombo M, et al. Synthesis and biological evaluation of 9-oxo-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile analogues as potential inhibitors of deubiquitinating enzymes. ChemMedChem. 2010 Apr 6;5(4):552-8.

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M443

发表于2024年5月6日由上海金畔生物科技有限公司

M443 纯度: 98.40%

M443 是 MRK 的一个不可逆的、特异性抑制剂，其 IC₅₀ 值 <125 nM。

M443 Chemical Structure

CAS No. : 1820684-31-8

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥5837	In-stock
5 mg	￥4500	In-stock
10 mg	￥7500	In-stock
25 mg	￥15000	In-stock
50 mg	￥21000	In-stock
100 mg	￥33000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

M443 相关产品

•相关化合物库:

Covalent Screening Library Plus
Bioactive Compound Library Plus
Anti-Cancer Compound Library
Covalent Screening Library
Targeted Diversity Library

生物活性

M443 is an irreversible and specific inhibitor of MRK, with an IC₅₀<125 nM.

IC₅₀ & Target

IC50: <125 nm (mrk)^[1].

体外研究
(In Vitro)

MRK depletion decreases cell viability after IR by 33% of control at 3 Gy. Similarly, the clonogenic assay shows a significant decrease in survival with a dose enhancement factor (DEF) of 1.6 at 10% viability. MRK activation by IR is maximal at 30 minutes after exposure to radiation. Therefore, for subsequent analysis, this time point is used. In both cell cultures, the IR-stimulated activation of MRK, Chk2, and p38 is greatly inhibited by 500 nM M443. Cells are seeded on coverslips, pretreated with 500 nM M443 or vehicle, exposed to 6 Gy of IR, fixed at different times after IR and processed for immunofluorescence with the MPM2 phospho-specific antibody that specifically stains mitotic cells. In contrast to control cells, the M443-treated cells fail to arrest after IR and maintained a similar mitotic index as the nonirradiated cells. Thus, inhibition of MRK leads to inhibition of Chk2 and failure to arrest in the cell cycle in response to IR-induced DNA damage^[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)

Control mice survive with a median of 32 days after tumor cell implantation. Treatment with M443 alone adds 5.5 days to this survival, whereas the chosen low dose of radiation does not significantly increase survival. In contrast, the combination of M443 and IR extend survival with a median of 16 days longer than control. Treatment with M443 does not affect the animal weight, as the weight loss observed is observed in all groups just a few days before the animals became moribund. It is showed that the tumor-containing fraction has elevated levels of both total and active MRK (lane RB in the vehicle-treated brain). In contrast, the tumor-containing fraction from the M443-treated brain shows total loss of MRK activity. Interestingly, the fractions containing normal brain, which in the control brain show some level of MRK protein, in the treated brain also has lost MRK, suggesting that diffusion of M443 across the whole cerebellum inhibit normal MRK as well^[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

589.61

Formula

C₃₁H₃₀F₃N₇O₂

CAS 号

1820684-31-8

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 : 55 mg/mL (93.28 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6960 mL	8.4802 mL	16.9604 mL
5 mM	0.3392 mL	1.6960 mL	3.3921 mL
10 mM	0.1696 mL	0.8480 mL	1.6960 mL

参考文献

[1]. Markowitz D, et al. Pharmacological Inhibition of the Protein Kinase MRK/ZAK Radiosensitizes Medulloblastoma. Mol Cancer Ther. 2016 Aug;15(8):1799-808.

Cell Assay ^[1]	Two days after transfection with siRNAs, medulloblastoma cells are seeded in a 96-well plate, and the following day, they are exposed to different doses of radiation. Cell viability is determined 72 hours after radiation treatment by MTT absorbance at 595 nm. For cells that are treated with M443 (250 nM, 500 nM), 6 hours after treatment with different concentrations of the drug or vehicle control, they are exposed to radiation and processed for the MTT assay 72 hours later as above. Five hundred cells are seeded in 6 cm dishes 2 days after siRNA transfections. The following day, cells are exposed to the different doses of radiation using a biologic irradiator and cultured for 7 days with media changes every other day. Colonies containing more than 50 cells are counted, and the results are used to calculate the surviving fractions. For the treatment with M443 or vehicle control, 24 hours after seeding, cells are exposed to the drug for 6 hours and subsequently to radiation^[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] The primary UI226 medulloblastoma cells are patient derived xenografts. UI226 is largely propagated as flank cultures in nude mice and cultured in StemPro media for less than 3 weeks before intracranial injections. Medulloblastoma cells (5.0×10⁵ UI226 in 5 mL of StemPro medium) are injected over 5 minutes into the cerebellum of 4-week-old athymic female mice. Three weeks after tumor cell implantation and approximately 2 weeks before the animals become moribund; treatment is started by implantation of an osmotic pump filled with either 0.05 mg/mL solution of M443 or vehicle (0.01% DMSO in PBS) and implanted in a subcutaneous pocket on the dorsal flank of the animal. A catheter with attached cannula delivers the drug intracranially and directly into the tumor over a period of 2 weeks, at a steady rate of 0.25 mL/hour. Irradiation of the mice head is initiated 2 days after pump implantation and conducted over 2 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.
参考文献	[1]. Markowitz D, et al. Pharmacological Inhibition of the Protein Kinase MRK/ZAK Radiosensitizes Medulloblastoma. Mol Cancer Ther. 2016 Aug;15(8):1799-808.

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ML346

发表于2024年4月14日由上海金畔生物科技有限公司

ML346 纯度: ≥98.0%

ML346是 Hsp70 和 HSF-1 活性的激活剂，针对 Hsp70 的 EC₅₀ 为 4.6 μM。ML346 恢复构象疾病模型中的蛋白质折叠，而没有明显的细胞毒性或缺乏特异性。ML346 诱导了热休克反应 (HSR) 的基因和蛋白质效应子的特异性增加，包括伴侣蛋白如 Hsp70，Hsp40 和 Hsp27。

ML346 Chemical Structure

CAS No. : 100872-83-1

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥898	In-stock
2 mg	￥600	In-stock
5 mg	￥990	In-stock
10 mg	￥1650	In-stock
50 mg	￥6600	In-stock
100 mg	￥9950	In-stock
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ML346 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Cell Cycle/DNA Damage Compound Library
Metabolism/Protease Compound Library
Anti-Cancer Compound Library
Anti-Aging Compound Library
Oxygen Sensing Compound Library
Cytoskeleton Compound Library

生物活性

ML346 is an activator of Hsp70 expression and HSF-1 activity, with an EC₅₀ of 4.6 μM for Hsp70. ML346 restores protein folding in conformational disease models, without significant cytotoxicity or lack of specificity. ML346 induces specific increases in genes and protein effectors of the heat shock response (HSR), including chaperones such as Hsp70, Hsp40, and Hsp27^[1].

IC₅₀ & Target^[1]

HSP70

4.6 μM (EC₅₀, HeLa cells)

体外研究
(In Vitro)

ML346 is an activator of Hsp70, with an EC₅₀ of 4600 nM in HeLa cells. ML346 (10 μM) restores proteostasis, restores CFTR-mediated iodide conductance, and enhances the correct folding of proteins expressed in two different cellular compartments^[1]. ML346 (Compound F1) induces multiple responses and strongly induces Hsp70, the oxidative stress response genes (HO1 and GCLM), and a 2.5-fold upregulation of BiP in WT MEF cells. ML346 (0.5-25 μM) exhibits cytoprotective effects in cells after a 35 min severe heat shock, and also causes a two-fold protection from H₂O₂-induced apoptosis^[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.

体内研究
(In Vivo)

ML346 suppress the aggregation of polyQ35 in a C. elegans model, suggesting the probe has efficacy in modifying protein aggregation and associated toxicity^[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

272.26

Formula

C₁₄H₁₂N₂O₄

CAS 号

100872-83-1

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 : 12.5 mg/mL (45.91 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.6730 mL	18.3648 mL	36.7296 mL
5 mM	0.7346 mL	3.6730 mL	7.3459 mL
10 mM	0.3673 mL	1.8365 mL	3.6730 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% (20% SBE-β-CD in saline)

Solubility: ≥ 1.25 mg/mL (4.59 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (4.59 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 12.5 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

*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]. Calamini B, et al. ML346: A Novel Modulator of Proteostasis for Protein Conformational Diseases.Probe Reports from the NIH Molecular Libraries Program. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. 2012 Dec 17.

[2]. Calamini B, et al. Small-molecule proteostasis regulators for protein conformational diseases. Nat Chem Biol. 2011 Dec 25;8(2):185-96.

Kinase Assay ^[2]	In brief, HeLa cells are incubated with either DMSO (negative control), the positive controls MG132 (10 μM) and lactacystin (6 μM) or the PRs A1, A3 and ML346 (F1) for 3 and 6 hours and then harvested. Cells are lysed in homogenization buffer (50 mM Tris-HCl, pH7.5, 250 mM sucrose, 5 mM MgCl₂, 2 mM ATP, 1 mM DTT, 0.5 mM EDTA, 0.025% digitonin) for 5 min on ice, and total protein concentration of whole cell extract is determined. 3 μg of whole cell extracts are combined with assay buffer (50 mM Tris-HCl, pH 7.5, 40 mM KCl, 5 mM MgCl₂, 0.5 mM ATP, 1 mM DTT, 0.05 mg/mL BSA) in a black 96-well plate and the reaction is initiated by the addition of a 2× (200 μM) fluorogenic peptide substrate Suc-LLVY-AMC. Fluorescence is measured every 10 min using a Synergy H4 multi-mode microplate reader^[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.
Cell Assay ^[2]	HeLa cells are plated at a density of 10,000 cells per well in black 96-well plates in 100 μL of DMEM supplemented with 10% FBS and 1% Pen/Strep/Neo. Plates are incubated for 16 hours at 37°C, 5% CO₂ and 95% relative humidity before compound addition. 1 μL of hit compounds (ML346) in DMSO or DMSO alone are added to the sample or control wells, respectively. Plates are then placed back in the incubator for 24 hours. After incubation, cells are washed 2× with 200 μL of PBS and 200 μL of a solution of 1 μg/mL of calcein AM is added to each well. Cells are then incubated for 45 min at 37°C, 5% CO₂ before fluorescence measurement using an Analyst GT multimode reader. Percent cytotoxicity is expressed relative to wells containing cells treated with DMSO only (100%)^[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.
参考文献	[1]. Calamini B, et al. ML346: A Novel Modulator of Proteostasis for Protein Conformational Diseases.Probe Reports from the NIH Molecular Libraries Program. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. 2012 Dec 17. [2]. Calamini B, et al. Small-molecule proteostasis regulators for protein conformational diseases. Nat Chem Biol. 2011 Dec 25;8(2):185-96.

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RI-2

发表于2024年4月10日由上海金畔生物科技有限公司

RI-2 纯度: 99.64%

RI-2 是一种可逆的 RAD51 抑制剂，IC₅₀ 值为 44.17 μM，能够特异性地抑制人体细胞中的同源重组修复。

RI-2 Chemical Structure

CAS No. : 1417162-36-7

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5 mg	￥2350	In-stock
10 mg	￥4000	In-stock
50 mg	￥12000	In-stock
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RI-2 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Cell Cycle/DNA Damage Compound Library
Anti-Cancer Compound Library
Anti-Aging Compound Library

生物活性

RI-2 is a reversible RAD51 inhibitor, with an IC₅₀ of 44.17 μM, and specifically inhibits homologous recombination repair in human cells.

IC₅₀ & Target

IC50: 44.17 μM (RAD51)^[1]

体外研究
(In Vitro)

RI-2 (7a) is a reversible RAD51 inhibitor, with an IC₅₀ of 44.17 μM. RI-2 specifically inhibits homologous recombination repair in human cells. RI-2 (150 μM) induces a significant sensitization of cells^[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

433.28

Formula

C₂₁H₁₈Cl₂N₂O₄

CAS 号

1417162-36-7

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 : 130 mg/mL (300.04 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3080 mL	11.5399 mL	23.0798 mL
5 mM	0.4616 mL	2.3080 mL	4.6160 mL
10 mM	0.2308 mL	1.1540 mL	2.3080 mL

参考文献

[1]. Budke B, et al. An optimized RAD51 inhibitor that disrupts homologous recombination without requiring Michael acceptor reactivity. J Med Chem. 2013 Jan 10;56(1):254-63.

Cell Assay
^[1]

HEK293 cells are plated into 96-well tissue culture plates at a density of 300 cells per well in the presence or absence of 50 nM mitomycin C (MMC) for 24 hours at 37°C, 5% CO₂. Media is subsequently replaced with fresh media containing 0.5% DMSO plus RI-2 for an additional 24 hours. RI-2 is then removed, and cultures are allowed to grow to a 50-70% confluence. Average survival from at least three replicates is measured using CellGlo reagentor. RI-2 is deemed successful in sensitizing cells to MMC if they generate significantly greater toxicity in the presence of MMC relative to the absence of MMC. Specifically, sensitization is scored as a “+” when non-overlapping standard errors are observed for at least two pairs of compound doses^[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]. Budke B, et al. An optimized RAD51 inhibitor that disrupts homologous recombination without requiring Michael acceptor reactivity. J Med Chem. 2013 Jan 10;56(1):254-63.

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USP7-IN-8

发表于2024年3月11日由上海金畔生物科技有限公司

USP7-IN-8 纯度: 98.80%

USP7-IN-8 (example 81) 是一种选择性的泛素特异性蛋白酶 7 (USP7) 抑制剂，在 Ub-Rho110 分析中的 IC₅₀ 为 1.4 μM。USP7-IN-8 对 USP47 和 USP5 没有活性。USP7-IN-8 具有抗癌作用。

USP7-IN-8 Chemical Structure

CAS No. : 2009273-60-1

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USP7-IN-8 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Cell Cycle/DNA Damage Compound Library
Anti-Cancer Compound Library
Anti-Aging Compound Library
Ubiquitination Compound Library

生物活性

USP7-IN-8 (example 81) is a selective ubiquitin-specific protease 7 (USP7) inhibitor with an IC₅₀ of 1.4 μM in an Ub-Rho110 assay. USP7-IN-8 shows no activity against USP47 and USP5. USP7-IN-8 has anticancer effects^[1].

IC₅₀ & Target

IC50: 1.4 μM (USP7)

体外研究
(In Vitro)

USP7 or HAUSP (herpesvirus-associated USP) is a ubiquitin specific protease or a deubiquitylating enzyme that cleaves ubiquitin from its substrates. USP7 is a eubiquitinase (DUB) that controls cell proliferation by altering the stability of Mdm2, p53, PTEN and FOXO4^[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

347.41

Formula

C₂₁H₂₁N₃O₂

CAS 号

2009273-60-1

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 : 83.33 mg/mL (239.86 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8784 mL	14.3922 mL	28.7844 mL
5 mM	0.5757 mL	2.8784 mL	5.7569 mL
10 mM	0.2878 mL	1.4392 mL	2.8784 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 (5.99 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.99 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 (5.99 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.99 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 (5.99 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.99 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]. Robert Blake, et al. Usp7 inhibitor compounds and methods of use. US20160272588A1.

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UNC4976

发表于2024年1月24日由上海金畔生物科技有限公司

UNC4976

UNC4976 是一种 CBX7 染色质结构域与核酸结合的正变构调节剂 (PAM) 拟肽。UNC4976 拮抗 H3K27me3 特异性募集 CBX7 至靶基因，同时增加与 DNA 和 RNA 的非特异性结合。

UNC4976 Chemical Structure

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生物活性	UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA^[1].
分子量	847.09
Formula	C₄₇H₇₀N₆O₈
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]. Lamb KN, et al. Discovery and Characterization of a Cellular Potent Positive Allosteric Modulator of the Polycomb Repressive Complex 1 Chromodomain, CBX7. Cell Chem Biol. 2019 Aug 14.

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UNC4976

发表于2024年1月24日由上海金畔生物科技有限公司

UNC4976

UNC4976 Chemical Structure

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

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生物活性	UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA^[1].
分子量	847.09
Formula	C₄₇H₇₀N₆O₈
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]. Lamb KN, et al. Discovery and Characterization of a Cellular Potent Positive Allosteric Modulator of the Polycomb Repressive Complex 1 Chromodomain, CBX7. Cell Chem Biol. 2019 Aug 14.

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UNC4976

发表于2024年1月24日由上海金畔生物科技有限公司

UNC4976

UNC4976 Chemical Structure

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

* Please select Quantity before adding items.

生物活性	UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA^[1].
分子量	847.09
Formula	C₄₇H₇₀N₆O₈
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]. Lamb KN, et al. Discovery and Characterization of a Cellular Potent Positive Allosteric Modulator of the Polycomb Repressive Complex 1 Chromodomain, CBX7. Cell Chem Biol. 2019 Aug 14.

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P53R3

发表于2023年12月28日由上海金畔生物科技有限公司

P53R3

P53R3 是一种有效的 p53 reactivator，可恢复 p53 热点突变体（包括 p53^R175H、p53^R248W 和 p53^R273H）的序列特异性 DNA 结合。P53R3 以比 PRIMA-1 高得多的特异性诱导 p53 依赖性抗增殖作用。P53R3 增强了野生型 p53 和 p53^M237I 向几个靶基因启动子的募集。 P53R3 强烈增强死亡受体死亡受体 5 (DR5) 的 mRNA、总蛋白和细胞表面表达。 P53R3 可以用于癌症研究。

P53R3 Chemical Structure

CAS No. : 922150-12-7

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生物活性

P53R3 is a potent p53 reactivator and restores sequence-specific DNA binding of p53 hot spot mutants, including p53^R175H, p53^R248W and p53^R273H. P53R3 induces p53-dependent antiproliferative effects with much higher specificity than PRIMA-1. P53R3 enhances the recruitment of wild-type p53 and p53^M237I to several target gene promoters. P53R3 strongly enhances the mRNA, total protein and cell surface expression of the death receptor death receptor 5 (DR5). P53R3 is used for cancer research^[1].

体外研究
(In Vitro)

P53R3 (10 μg/ml; 24 hours; in the absence or presence of the unlabelled p53 consensus oligonucleotide) restores p53-specific DNA binding activity to p53^R273H (a DNA contact mutant) and p53R175H (a structural mutant) in WiDr colon tumour cells harbouring p53^R273H and KLE cells with p53R175H^[1].
P53R3 (1-33 μg/ml; 24 hours) inhibits the proliferation of the LN-308 sublines expressing mutant p53 plasmids in a p53-dependent manner. The p53^R175H-dependent effects are strong over a broad range of concentrations, but p53^R273H-dependent effects are weaker and requires high concentrations of P53R3^[1].
P53R3 induces p53^R248W reactivation is more pronounced proliferation inhibition than observed with p53^R273H. P53R3 does not exhibit cytotoxic effects even at concentrations close to its solubility limit (33 μg/ml)^[1].
P53R3 (33 μg/ml; 18 hours) induces a strong decrease in S phase cells and a G0/G1 cell cycle arrest in LN-308 p53^R175H and LN-308 p53^R273H cells. But it does not affect cell cycle distribution of LN-308 p53^R248W cells^[1].

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

Cell Viability Assay^[1]

Cell Line:	p53 null LN-308 human glioma cells with a control plasmid or plasmids encoding the mutants p53R175H, p53R248W and p53R273H
Concentration:	1-33 μg/mL
Incubation Time:	24 hours
Result:	Induced p53-dependent and -independent antiproliferative and cytotoxic effects in vitro.

分子量

592.56

Formula

C₃₂H₃₅Cl₂N₅O₂

CAS 号

922150-12-7

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]. Alejandro Parrales, et al. Targeting Oncogenic Mutant p53 for Cancer Therapy. Front Oncol

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P53R3

发表于2023年12月28日由上海金畔生物科技有限公司

P53R3

P53R3 Chemical Structure

CAS No. : 922150-12-7

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

* Please select Quantity before adding items.

生物活性

体外研究
(In Vitro)

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 Viability Assay^[1]

Cell Line:	p53 null LN-308 human glioma cells with a control plasmid or plasmids encoding the mutants p53R175H, p53R248W and p53R273H
Concentration:	1-33 μg/mL
Incubation Time:	24 hours
Result:	Induced p53-dependent and -independent antiproliferative and cytotoxic effects in vitro.

分子量

592.56

Formula

C₃₂H₃₅Cl₂N₅O₂

CAS 号

922150-12-7

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]. Alejandro Parrales, et al. Targeting Oncogenic Mutant p53 for Cancer Therapy. Front Oncol

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P53R3

发表于2023年12月28日由上海金畔生物科技有限公司

P53R3

P53R3 Chemical Structure

CAS No. : 922150-12-7

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

* Please select Quantity before adding items.

生物活性

体外研究
(In Vitro)

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

Cell Viability Assay^[1]

Cell Line:	p53 null LN-308 human glioma cells with a control plasmid or plasmids encoding the mutants p53R175H, p53R248W and p53R273H
Concentration:	1-33 μg/mL
Incubation Time:	24 hours
Result:	Induced p53-dependent and -independent antiproliferative and cytotoxic effects in vitro.

分子量

592.56

Formula

C₃₂H₃₅Cl₂N₅O₂

CAS 号

922150-12-7

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]. Alejandro Parrales, et al. Targeting Oncogenic Mutant p53 for Cancer Therapy. Front Oncol

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