I-CBP112 hydrochloride

发表于2024年11月1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。

I-CBP112 hydrochloride

I-CBP112 盐酸盐是一种选择性的 CBP/P300 抑制剂，可直接结合它们的溴结构域 (K_ds分别为 142 和 625 nM)。在体外和体内，I-CBP112 以剂量依赖性方式显著降低 MLL-AF9(+) 急性髓系白血病细胞的白血病启动潜能。I-CBP112 增加 BET 抑制剂 JQ1 和阿霉素的细胞毒性。

I-CBP112 hydrochloride Chemical Structure

CAS No. : 2147701-33-3

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生物活性	I-CBP112 hydrochloride is a selective inhibitor of CBP/P300 that directly binds their bromodomains (K_ds = 142 and 625 nM, respectively). I-CBP112 significantly reduces the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells in a dose-dependent manner in vitro and in vivo. I-CBP112 increases the cytotoxic activity of BET bromodomain inhibitor JQ1 as well as doxorubicin^[1].
分子量	505.05
Formula	C₂₇H₃₇ClN₂O₅
CAS 号	2147701-33-3
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]. Picaud S, et al. Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy. Cancer Res. 2015 Dec 1;75(23):5106-5119.

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CBP/p300-IN-12

发表于2024年10月29日由上海金畔生物科技有限公司

CBP/p300-IN-12

CBP/p300-IN-12 是一种有效的选择性共价组蛋白乙酰转移酶 p300 (IC₅₀ 为 166 nM) 和 CBP 抑制剂。CBP/p300-IN-12 降低 PC-3 细胞的 H3K27Ac 水平 (EC₅₀ 为 37 nM)。CBP/p300-IN-12 可与 C1450 形成共价加合物。

CBP/p300-IN-12 Chemical Structure

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生物活性	CBP/p300-IN-12 is a potent and selective covalent histone acetyltransferases p300 (IC₅₀ of 166 nM) and CBP inhibitor. CBP/p300-IN-12 decreases the levels of H3K27Ac of PC-3 cells (EC₅₀ of 37 nM). CBP/p300-IN-12 forms a covalent adduct with C1450^[1].
IC₅₀ & Target	IC50: 166 nM (p300 HAT domain)^[1]
体外研究 (In Vitro)	CBP/p300-IN-12 (Compound 2) shows antiproliferative effect against androgen receptor (AR)-positive LnCaP-FGC cells (EC₅₀ of 87 nM), while displaying significantly less activity in the AR-negative cell line DU-145 (EC₅₀ of 1.37 μM). 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	667.61
Formula	C₃₃H₂₉F₄N₅O₆
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]. Anthony Mastracchio, et al. Discovery of a Potent and Selective Covalent p300/CBP Inhibitor. ACS Med Chem Lett. 2021 Apr 5;12(5):726-731.

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I-CBP112

发表于2024年10月18日由上海金畔生物科技有限公司

I-CBP112 纯度: 98.46%

I-CBP112是一种特异性和有效的乙酰-赖氨酸竞争性蛋白-蛋白相互作用抑制剂，抑制 CBP/p300 溴结构域，增强 p300 的乙酰化作用。

I-CBP112 Chemical Structure

CAS No. : 1640282-31-0

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥2887	In-stock
1 mg	￥1000	In-stock
5 mg	￥2800	In-stock
10 mg	￥5000	In-stock
50 mg		询价
100 mg		询价

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I-CBP112 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
Chemical Probe Library
Anti-Blood Cancer Compound Library

生物活性

I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor, that inhibits the CBP/p300 bromodomains, enhances acetylation by p300.

IC₅₀ & Target

IC50: 5.5±1.1 μM (CBP/p300, Leukemia cell); 9.1±1.2 μM (CBP/p300, Prostate cancer cell)^[1]

体外研究
(In Vitro)

I-CBP112 significantly enhances acetylation by p300 at the histone H3K18 and H3K23 sites. I-CBP112 stimulated H3K18ac by ~3-fold, I-CBP112 induced enhances acetylation of these same sites by CBP as well as at H4K5. The EC₅₀’s of activation of I-CBP112 on p300- and CBP-mediated H3K18 acetylation are ~2 μM^[1]. Exposure of human and mouse leukemic cell lines to I-CBP112 results in substantially impaired colony formation and induces cellular differentiation without significant cytotoxicity. Exposure of the BioMAP primary cell panel to I-CBP112 results in a unique response on cytokine and marker protein expression^[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)

I-CBP112 significantly reduces the leukemia-initiating potential of mLL-AF9+ AmL cells in a dose-dependent manner in vitro and in vivo. The synergistic effects of I-CBP112 and current standard therapy (doxorubicin) as well as emerging treatment strategies (BET inhibition) provide new opportunities for combinatorial treatment of leukemia and potentially other cancers^[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

468.59

Formula

C₂₇H₃₆N₂O₅

CAS 号

1640282-31-0

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 : ≥ 32 mg/mL (68.29 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	2.1341 mL	10.6703 mL	21.3406 mL
5 mM	0.4268 mL	2.1341 mL	4.2681 mL
10 mM	0.2134 mL	1.0670 mL	2.1341 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 (5.34 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.34 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 (5.34 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.34 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 (5.34 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.34 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]. Zucconi BE, et al. Modulation of p300/CBP Acetylation of Nucleosomes by Bromodomain LigandI-CBP112. Biochemistry. 2016 Jul 12;55(27):3727-34.

[2]. Picaud S, et al. Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy. Cancer Res. 2015 Dec 1;75(23):5106-19.

Cell Assay ^[1]	I-CBP112 is dissolved in DMSO and diluted with appropriate medium before use. Cells (6000 KG1a and 13000 LNCaP cells/well) are plated in 96-well flat-bottom plates approximately 24 h prior to drug treatment. After 24 h, 10–20% fetal bovine serum-containing medium is replaced with 2.5% serum medium, and cells are treated with I-CBP112 in 0.18% DMSO; 0.18% DMSO is shown to have negligible cell growth effects under the conditions used in our experiments. After being exposed to I-CBP112 for 66 h, cells are subjected to a final concentration of 0.476% [3H]thymidine per well and allowed to proliferate for an additional 6 h (exposure to I-CBP112 for a total of 72 h). Cells are harvested, and the counts of 3H in each well are taken relative to those treated with vehicle alone to quantify the effect of the ligand on 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.
Animal Administration ^[2]	Mice: Leukemic blasts expressing MLL-AF9 are treated in liquid culture with 5 μM of I-CBP112 for 3 days. Control cells are exposed to the corresponding concentration of the DMSO vehicle. Treated cells are then transplanted into sublethally irradiated syngeneic mice via tail vein injection. Upon the development of signs of disease the mice are sacrificed and analysed^[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]. Zucconi BE, et al. Modulation of p300/CBP Acetylation of Nucleosomes by Bromodomain LigandI-CBP112. Biochemistry. 2016 Jul 12;55(27):3727-34. [2]. Picaud S, et al. Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy. Cancer Res. 2015 Dec 1;75(23):5106-19.

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NiCur

发表于2024年10月3日由上海金畔生物科技有限公司

NiCur 纯度: 99.09%

NiCur 是一种有效的选择性 CBP histone acetyltransferase (HAT) 抑制剂，其 IC₅₀ 值为 0.35 μΜ。NiCur 阻断 CBP HAT 活性，下调基因毒性应激时 p53 的激活。 NiCur 可用于不影响靶蛋白表达的机制研究。

NiCur Chemical Structure

规格	价格	是否有货
5 mg	￥2000	In-stock
10 mg	￥3500	In-stock
25 mg	￥6500	In-stock
50 mg	￥9500	In-stock
100 mg		询价
200 mg		询价

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NiCur 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

生物活性

NiCur is a potent and selective CBP histone acetyltransferase (HAT) inhibitor with an IC₅₀ value of 0.35 μΜ. NiCur, which blocks CBP HAT activity and downregulates p53 activation upon genotoxic stress. NiCur can be used for performing mechanistic studies without affecting the expression of target proteins^[1].

IC₅₀ & Target^[1]

CBP

0.35 μM (IC₅₀)

体外研究
(In Vitro)

NiCur (0.5~1 μM; U2OS cells) reduces the Dox-induced p53K382ac, p53S15p, and p53 levels in a dose-dependent manner^[1].
NiCur (1.5 μM) reduces the level of H3K27ac. NiCur (1.5 μM; U2OS cells) restores cellular proliferation. NiCur (Intestinal epithelial cells) down-regulates Dox-mediated p53 activation without affecting the levels of H2A.X S139p. NiCur can modulate the gene regulatory switch for reprogramming chromatin landscape. NiCur blocks CBP HAT activity^[1].

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

Western Blot Analysis^[1]

Cell Line:	U2OS cells
Concentration:	0.5~1 μM
Incubation Time:
Result:	Reduced the Dox-induced p53K382ac, p53S15p, and p53 levels in a dose-dependent manner.

分子量

324.38

Formula

C₂₂H₁₆N₂O

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 (154.14 mM; ultrasonic and warming 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	3.0828 mL	15.4140 mL	30.8280 mL
5 mM	0.6166 mL	3.0828 mL	6.1656 mL
10 mM	0.3083 mL	1.5414 mL	3.0828 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 (5.15 mM); Clear solution

此方案可获得 ≥ 1.67 mg/mL (5.15 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 (5.15 mM); Suspended solution; Need ultrasonic

此方案可获得 1.67 mg/mL (5.15 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 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

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

参考文献

[1]. Vincek AS, et al. Inhibitor of CBP Histone Acetyltransferase Downregulates p53 Activation and Facilitates Methylation at Lysine 27 on Histone H3. Molecules. 2018;23(8):1930. Published 2018 Aug 2.

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SGC-CBP30

发表于2024年10月1日由上海金畔生物科技有限公司

SGC-CBP30 纯度: 99.82%

SGC-CBP30 是一种有效且高度选择性的 CBP/p300 溴结构域抑制剂 (对 CBP 和 p300 的 K_d 值分别为 21 nM 和 32 nM)，其选择性是 BRD4 [BRD4(1)] 的 40 倍。SGC-CBP30 强烈减少 Th17 细胞中 IL-17A 的分泌，并具有抗炎作用。

SGC-CBP30 Chemical Structure

CAS No. : 1613695-14-9

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1407	In-stock
2 mg	￥837	In-stock
5 mg	￥1256	In-stock
10 mg	￥1469	In-stock
50 mg	￥4985	In-stock
100 mg	￥9650	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

SGC-CBP30 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Epigenetics Compound Library
Immunology/Inflammation Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Chemical Probe Library
Anti-Blood Cancer Compound Library

生物活性

SGC-CBP30 is a potent and highly selective CBP/p300 bromodomain (K_ds of 21 nM and 32 nM for CBP and p300, respectively) inhibitor, displaying 40-fold selectivity over the first bromodomain of BRD4 [BRD4(1)] bound. SGC-CBP30 strongly reduces secretion of IL-17A in Th17 cells and has anti-inflammatory effects^[1]^[2]^[3].

IC₅₀ & Target

CBP/p300 bromodomain^[1]^[3]

体外研究
(In Vitro)

In ankylosing spondylitis and psoriatic arthritis condition, SGC-CBP30 inhibits IL-17A secretion by Th17 cells. Transcriptional profiling of human T cells after SGC-CBP30 treatment shows a much more restricted effect on gene expression than that observed with the pan-BET (bromo and extraterminal domain protein family) bromodomain inhibitor JQ1^[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)

SGC-CBP30 treatment slightly alleviates alveolar bronchial fibrosis induced by NSC-125066. SGC-CBP30 plus CQ-061 dramatically reduces alveolar bronchial fibrosis. The ELISA of cytokines IL-4 and IFN-γ in BALF demonstrates that combination of SGC-CBP300 and CQ-061 suppresses the activation of IL-4 as well as IFN-γ in NSC-125066 induced IPF murine models to nearly normal levels^[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:	Sprague-Dawley (SD) rats (aged 3-4 weeks) injected with NSC-125066^[2]
Dosage:	25 mg/kg
Administration:	Oral administration; daily; for 14 days
Result:	Slightly alleviated alveolar bronchial fibrosis induced by NSC-125066.

分子量

509.04

Formula

C₂₈H₃₃ClN₄O₃

CAS 号

1613695-14-9

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 (60.90 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	1.9645 mL	9.8224 mL	19.6448 mL
5 mM	0.3929 mL	1.9645 mL	3.9290 mL
10 mM	0.1964 mL	0.9822 mL	1.9645 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 (4.91 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.91 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 (4.91 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.91 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]. Hammitzsch A, et al. CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses. Proc Natl Acad Sci U S A. 2015 Aug 25;112(34):10768-73.

[2]. Tao J, Inhibition of EP300 and DDR1 synergistically alleviates pulmonary fibrosis in vitro and in vivo. Biomed Pharmacother. 2018 Oct;106:1727-1733.

[3]. Hay DA, et al. Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains. J Am Chem Soc. 2014 Jul 2;136(26):9308-19.

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GNE-272

发表于2024年9月15日由上海金畔生物科技有限公司

GNE-272 纯度: 99.74%

GNE-272 是有效和选择性的 CBP/EP300 抑制剂，对 CBP，EP300 和 BRD4 的 IC₅₀ 值分别为0.02，0.03 和 13 μM。GNE-272 也是 CBP/EP300 选择性的体内探针。

GNE-272 Chemical Structure

CAS No. : 1936428-93-1

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1774	In-stock
2 mg	￥1100	In-stock
5 mg	￥1900	In-stock
10 mg	￥3000	In-stock
50 mg	￥12000	In-stock
100 mg	￥19000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

GNE-272 相关产品

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Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Chemical Probe Library
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生物活性

GNE-272 is a potent and selective CBP/EP300 inhibitor with IC₅₀ values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300^[1].

IC₅₀ & Target

IC50: 0.02 μM (CBP), 0.03 μM (EP300), 13 μM (BRD4)^[1]

体外研究
(In Vitro)

GNE-272 is exquisitely selective for CBP/ EP300 and remarkably selective (650-fold) over BRD4. When tested at 10 μM in 35 kinase panel and 42 receptors off-target screening panel, GNE-272 does not inhibit any target at >30%. In addition, GNE-272 does not inhibit (>10 μM, top concentration) several cytochrome P450s (3A4, 1A2, 2C9, 2C19, 2D6). The compound has good potency in the BRET cellular assay. In an orthogonal measure of the target engagement, GNE-272 is shown to inhibit the expression of MYC10 (MV4−11 cell line) with an EC₅₀ of 0.91 μM and good correlation between the BRET and MYC cellular assays is 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.

体内研究
(In Vivo)

GNE-272 demonstrates low clearance following a 1 mg/ kg intravenous dose in a mouse PK experiment and good oral bioavailability when dosed at 100 mg/kg, reaching an unbound C_max of 26 μM. GNE-272 shows a marked antiproliferative effect in hematologic cancer cell lines and modulates MYC expression in vivo that corresponds with antitumor activity in an AML tumor model^[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

424.47

Formula

C₂₂H₂₅FN₆O₂

CAS 号

1936428-93-1

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 : 100 mg/mL (235.59 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3559 mL	11.7794 mL	23.5588 mL
5 mM	0.4712 mL	2.3559 mL	4.7118 mL
10 mM	0.2356 mL	1.1779 mL	2.3559 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 (5.89 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.89 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 (5.89 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.89 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 (5.89 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.89 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]. Crawford TD, et al. Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300. J Med Chem. 2016 Dec 8;59(23):10549-10563.

Cell Assay ^[1]	Human cancer cell lines (MOLM-16, HL-60, LP-1, KMS-34, Pfeiffer, DOHH-2) are treated for 4 h with 5 μM GNE-272 or DMSO control. After 6 days, cell viability is measured by CellTiter-Glo^[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: Mice are given 0 (vehicle, 0.5% methylcellulose; 0.2% Tween-80), 12.5, 25, and 50 mg/kg of GNE-272 by gavage, twice daily (BID) for 21 days in a volume of 100 μL. Tumor volumes are measured in two dimensions (length and width) using Ultra CalIV calipers and analyzed using Excel, version 11.2^[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]. Crawford TD, et al. Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300. J Med Chem. 2016 Dec 8;59(23):10549-10563.

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CBP/p300-IN-5

发表于2024年7月22日由上海金畔生物科技有限公司

CBP/p300-IN-5

P300/CBP-IN-5 是一种有效的 p300/CBP 组蛋白乙酰转移酶 (histone acetyltransferase) 抑制剂，其 IC₅₀ 值为 18.8 nM。详细信息请参考专利文献 WO2016044770A1 中的 Example 715。

CBP/p300-IN-5 Chemical Structure

CAS No. : 1889284-33-6

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生物活性	P300/CBP-IN-5 is a potent p300/CBP histone acetyltransferase inhibitor extracted from patent WO2016044770A1, Example 715, has an IC₅₀ of 18.8 nM^[1].
IC₅₀ & Target	IC50: 18.8 nM (p300/CBP)^[1]
体外研究 (In Vitro)	P300/CBP-IN-5 inhibits p300 LnCap-FGC cellls proliferation with an IC₅₀ of 14.8 nM. P300/CBP-IN-5 inhibits H3K27Ac with an IC₅₀ value of 4.6 nM in PC-3 cells^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)	The effect of P300/CBP-IN-5 (Example 715) on tumor growth is evaluated in subcutaneous, SuDHL-8 (B-cell lymphoma) and 22RV1 (prostate) xenograft tumors implanted in SCID female mice. Human cancer cells are inoculated subcutaneously into the right hind flank of female SCID mice on study day 0. Administration of P300/CBP-IN-5 (7.5 mg/kg/day) is initiated at the time of size match. P300/CBP-IN-5 induces significant tumor growth inhibition in multiple xenograft tumor models (the tumor growth inhibition of 62% in SuDHL-8 xenograft tumor model; 48% in 22RV1 xenograft tumor model)^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	618.55
Formula	C₂₉H₂₇F₅N₆O₄
CAS 号	1889284-33-6
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]. Michael Michaelides, et al. Spirocyclic hat inhibitors and methods for their use. WO2016044770A1.

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Thalidomide-NH-CBP/p300 ligand 2

发表于2024年5月11日由上海金畔生物科技有限公司

Thalidomide-NH-CBP/p300 ligand 2 纯度: 99.85%

Thalidomide-NH-CBP/p300 ligand 2 (P-007) 是 CBP 和 p300 的 PROTAC 降解剂。

Thalidomide-NH-CBP/p300 ligand 2 Chemical Structure

CAS No. : 2484739-21-9

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5 mg	￥10500	In-stock
10 mg	￥16500	In-stock
50 mg		询价
100 mg		询价

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Thalidomide-NH-CBP/p300 ligand 2 相关产品

•相关化合物库:

Bioactive Compound Library Plus

生物活性

Thalidomide-NH-CBP/p300 ligand 2 (P-007) is a PROTAC-based CBP and p300 degrader (extracted from patent WO2020173440)^[1].

分子量

922.03

Formula

C₄₈H₅₇F₂N₁₁O₆

CAS 号

2484739-21-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据

In Vitro:

DMSO : 113.33 mg/mL (122.91 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.0846 mL	5.4228 mL	10.8456 mL
5 mM	0.2169 mL	1.0846 mL	2.1691 mL
10 mM	0.1085 mL	0.5423 mL	1.0846 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 (sealed storage, away from moisture and 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。

参考文献

[1]. LIU JING, et al. CYCLIC-AMP RESPONSE ELEMENT BINDING PROTEIN (CBP) AND/OR ADENOVIRAL E1A BINDING PROTEIN OF 300 KDA (P300) DEGRADATION COMPOUNDS AND METHODS OF USE. Patent WO2020173440.

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CPI-637

发表于2024年5月7日由上海金畔生物科技有限公司

CPI-637 纯度: 99.91%

CPI-637 是一种选择性和有效的 CBP/EP300 溴结构域抑制剂，其对 CBP, EP300 和 BRD4 BD-1 的 IC₅₀ 值分别为 0.03 μM，0.051 μM 和 11.0 μM，对 CBP 的 EC₅₀ 值为 0.3 μM。

CPI-637 Chemical Structure

CAS No. : 1884712-47-3

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Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥880	In-stock
5 mg	￥800	In-stock
10 mg	￥1100	In-stock
50 mg	￥3900	In-stock
100 mg	￥7200	In-stock
200 mg		询价
500 mg		询价

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CPI-637 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
Chemical Probe Library
Anti-Blood Cancer Compound Library
Targeted Diversity Library

生物活性

CPI-637 is a selective and potent CBP/EP300 bromodomain inhibitor with IC₅₀ values of 0.03 μM, 0.051 μM and 11.0 μM for CBP, EP300 and BRD4 BD-1, respectively, and an EC₅₀ of 0.3 μM for CBP^[1].

IC₅₀ & Target

BRD4 BD1

11 μM (IC₅₀)

CBP

0.03 μM (IC₅₀)

EP300

0.051 μM (IC₅₀)

CBP

0.3 μM (EC₅₀)

体外研究
(In Vitro)

CPI-637 (Compound 28) inhibits MYC expression in AMO-1 cells (EC₅₀ value of 0.60 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

386.45

Formula

C₂₂H₂₂N₆O

CAS 号

1884712-47-3

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 : 9.62 mg/mL (24.89 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5877 mL	12.9383 mL	25.8766 mL
5 mM	0.5175 mL	2.5877 mL	5.1753 mL
10 mM	0.2588 mL	1.2938 mL	2.5877 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: ≥ 0.96 mg/mL (2.48 mM); Clear solution

此方案可获得 ≥ 0.96 mg/mL (2.48 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 9.6 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: 0.96 mg/mL (2.48 mM); Suspended solution; Need ultrasonic

此方案可获得 0.96 mg/mL (2.48 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 9.6 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: ≥ 0.96 mg/mL (2.48 mM); Clear solution

此方案可获得 ≥ 0.96 mg/mL (2.48 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 9.6 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]. Taylor AM, et al. Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637). ACS Med Chem Lett. 2016 Mar 15;7(5):531-6.

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CBP/p300-IN-1

发表于2024年4月27日由上海金畔生物科技有限公司

CBP/p300-IN-1 纯度: 99.84%

CBP/p300-IN-1 是 CBP/EP300 溴结构域抑制剂。

CBP/p300-IN-1 Chemical Structure

CAS No. : 2443789-32-8

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
5 mg	￥2500	In-stock
10 mg	￥4000	In-stock
25 mg	￥8000	In-stock
50 mg	￥14000	In-stock
100 mg		询价
200 mg		询价

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CBP/p300-IN-1 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

CBP/p300-IN-1 is a CBP/EP300 bromodomain inhibitor.

IC₅₀ & Target

CBP/EP300^[1]

分子量

426.44

Formula

C₂₃H₂₃FN₂O₅

CAS 号

2443789-32-8

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 : 62.5 mg/mL (146.56 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3450 mL	11.7250 mL	23.4500 mL
5 mM	0.4690 mL	2.3450 mL	4.6900 mL
10 mM	0.2345 mL	1.1725 mL	2.3450 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 (4.88 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.88 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% corn oil

Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.88 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]. Xiang Q, et al. Discovery and optimization of 1-(1H-indol-1-yl)ethanone derivatives as CBP/EP300 bromodomain inhibitors for the treatment of castration-resistant prostate cancer. Eur J Med Chem. 2018 Mar 10;147:238-252.

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CBP/p300-IN-8

发表于2024年3月13日由上海金畔生物科技有限公司

CBP/p300-IN-8 纯度: 99.88%

CBP/p300-IN-8 是 CBP/P300 溴结构域家族的有效抑制剂。CBP/p300-IN-8 抑制 CBP (IC₅₀=0.01-0.1 µΜ) 和 BRD4 (IC₅₀=1-1000 µΜ) 活性。

CBP/p300-IN-8 Chemical Structure

CAS No. : 2304416-91-7

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5 mg	￥7800	In-stock
10 mg	￥12500	In-stock
50 mg	￥36500	In-stock
100 mg		询价
200 mg		询价

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CBP/p300-IN-8 相关产品

•相关化合物库:

Bioactive Compound Library Plus

生物活性

CBP/p300-IN-8 is a potent inhibitor of the CBP/P300 family of bromodomains. CBP/p300-IN-8 inhibits CBP (IC₅₀=0.01-0.1 µΜ) and BRD4 (IC₅₀=1-1000 µΜ) activity^[1].

IC₅₀ & Target^[1]

CBP

0.01-0.1 μM (IC₅₀)

BRD4

1-1000 μM (IC₅₀)

分子量

461.55

Formula

C₂₇H₃₁N₃O₄

CAS 号

2304416-91-7

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 : 200 mg/mL (433.32 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1666 mL	10.8331 mL	21.6661 mL
5 mM	0.4333 mL	2.1666 mL	4.3332 mL
10 mM	0.2167 mL	1.0833 mL	2.1666 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: ≥ 5 mg/mL (10.83 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (10.83 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]. Shawn E.R. Schiller, et al. Tetrahydro-imidazo quinoline compositions as cbp/p300 inhibitors. WO2019055877A1.

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CBP/p300-IN-2

发表于2024年3月13日由上海金畔生物科技有限公司

CBP/p300-IN-2

CBP/EP300-IN-2 是 CBP/EP300 的抑制剂，结合 CBP/HTRF 和 Myc，IC₅₀ 值分别为 1.07 nM 和 5.96 nM。CBP/EP300-IN-2，例 25，源于专利文献 WO2017205538A1。

CBP/p300-IN-2 Chemical Structure

CAS No. : 2158265-96-2

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500 mg		询价

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生物活性	CBP/EP300-IN-2 is an inhibitor of CBP/EP300 with IC₅₀ values of 1.07 nM and 5.96 nM for CBP/HTRF and Myc, respectively. CBP/EP300-IN-2, example 25, is extracted from patent WO2017205538A1^[1].
IC₅₀ & Target	IC50:1.07 nM (CBP/HTRF); 5.96 nM (Myc)^[1]
分子量	521.56
Formula	C₂₇H₂₉F₂N₇O₂
CAS 号	2158265-96-2
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]. Patrick Cyr, et al. Pyrazolopyridine derivatives for the treatment of cancer

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CBP/p300-IN-3

发表于2024年3月7日由上海金畔生物科技有限公司

CBP/p300-IN-3 纯度: 98.23%

CBP/p300-IN-3, a p300/CBP 组蛋白乙酰转移酶 (histone acetyltransferase) 抑制剂，化合物 6，来源于专利 WO 2019049061 A1。

CBP/p300-IN-3 Chemical Structure

CAS No. : 2299226-01-8

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥3300	In-stock
5 mg	￥3000	In-stock
10 mg	￥5000	In-stock
50 mg	￥14500	In-stock
100 mg		询价

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CBP/p300-IN-3 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

生物活性

CBP/p300-IN-3, a p300/CBP histone acetyltransferase inhibitor, Compound 6, is sourced from patent WO 2019049061 A1^[1].

分子量

431.53

Formula

C₂₄H₂₉N₇O

CAS 号

2299226-01-8

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 : 250 mg/mL (579.33 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3173 mL	11.5867 mL	23.1734 mL
5 mM	0.4635 mL	2.3173 mL	4.6347 mL
10 mM	0.2317 mL	1.1587 mL	2.3173 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 (4.82 mM); Clear solution

此方案可获得 ≥ 2.08 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 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 (4.82 mM); Clear solution

此方案可获得 ≥ 2.08 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 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 (4.82 mM); Clear solution

此方案可获得 ≥ 2.08 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 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]. Medina, et al. 5-(1H-Benzo[d]imidazol-2-yl)pyridin-2-amine and 5-(3H-imidazo[4,5-b]pyridin-6-yl)pyridin-2-amine derivatives as c-MYC and p300/CBP histone acetyltransferase inhibitors for treating cancer and their preparation.

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PROTAC CBP/P300 Degrader-1

发表于2024年3月4日由上海金畔生物科技有限公司

PROTAC CBP/P300 Degrader-1 纯度: 99.18%

PROTAC CBP/P300 Degrader-1 是一种有效的 PROTAC CBP/P300 降解剂。PROTAC CBP/P300 Degrader-1 有效抑制多个癌细胞系的细胞活力。

PROTAC CBP/P300 Degrader-1 Chemical Structure

CAS No. : 2484739-48-0

规格	价格	是否有货
5 mg	￥10500	In-stock
10 mg	￥16500	In-stock
50 mg		询价
100 mg		询价

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PROTAC CBP/P300 Degrader-1 相关产品

•相关化合物库:

Bioactive Compound Library Plus

生物活性

PROTAC CBP/P300 Degrader-1 is a potent PROTAC CBP/P300 degrader. PROTAC CBP/P300 Degrader-1 potently inhibited cell viability of multiple cancer cell lines^[1].

IC₅₀ & Target^[1]

Cereblon

体外研究
(In Vitro)

PROTAC CBP/P300 Degrader-1 shows LNCaP prostate cancer cell viability inhibition (IC₅₀=0.4 nM). PROTAC CBP/P300 Degrader-1 (10 nM) induces degradation of P300 (≥ 80%)^[1].
PROTAC CBP/P300 Degrader-1 potently inhibited cell viability of multiple cancel cell lines (IC₅₀s ranging from 0.1-141.4 nM for HEL, NOMO-1, MOLM-13, HL-60, MEG-01, MM.IS, MM.1R, NCL-H929, RPM-8226, AMO-1, WSU-DLCL2, Karpas-422, Pfeiffer, SU-DHL-1, LNCap clone FGC, VCap; 22RV1, NCI-H520, NCI-H703, LK-2, 上海金畔生物科技有限公司-7, and SK-BR-3 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

893.98

Formula

C₄₆H₅₃F₂N₁₁O₆

CAS 号

2484739-48-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据

In Vitro:

DMSO : 173.33 mg/mL (193.89 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.1186 mL	5.5930 mL	11.1859 mL
5 mM	0.2237 mL	1.1186 mL	2.2372 mL
10 mM	0.1119 mL	0.5593 mL	1.1186 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: 6.5 mg/mL (7.27 mM); Suspended solution; Need ultrasonic

此方案可获得 6.5 mg/mL (7.27 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 65.0 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

*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]. Jing Liu, et al. Cyclic-amp response element binding protein (cbp) and/or adenoviral e1a binding protein of 300 kda (p300) degradation compounds and methods of use. WO2020173440A1.

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TPOP146

发表于2024年2月28日由上海金畔生物科技有限公司

TPOP146 纯度: 99.66%

TPOP146是选择性的CBP/P300苯并西泮溴结构域抑制剂；对CBP和BRD4的K_d值分别为134 nM和5.02 μM。

TPOP146 Chemical Structure

CAS No. : 2018300-62-2

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1110	In-stock
5 mg	￥1050	In-stock
10 mg	￥1800	In-stock
50 mg	￥4800	In-stock
100 mg	￥8000	In-stock
200 mg		询价
500 mg		询价

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TPOP146 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

TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with K_d values of 134 nM and 5.02 μM for CBP and BRD4.

IC₅₀ & Target

IC50: 134 nM (CBP); 5.02 μM (BRD4)^[1]

体外研究
(In Vitro)

Exposure to 1 μM TPOP146 results in a significant decrease of recovery half-life that is comparable to the construct that contained the bromodomain inactivating mutation N1168F, demonstrating that TPOP146 targets the CBP bromodomain in the nucleus and is capable of competing with acetyl-lysine mediated interactions of the CBP bromodomain in cellular environments^[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

481.58

Formula

C₂₇H₃₅N₃O₅

CAS 号

2018300-62-2

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 : ≥ 100 mg/mL (207.65 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	2.0765 mL	10.3825 mL	20.7650 mL
5 mM	0.4153 mL	2.0765 mL	4.1530 mL
10 mM	0.2076 mL	1.0382 mL	2.0765 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 (5.19 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.19 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 (5.19 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.19 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 (5.19 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.19 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]. Popp TA, et al. Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors. J Med Chem. 2016 Oct 13;59(19):8889-8912.

Kinase Assay
^[1]

Proteins are buffered in 10 mM HEPES, pH 7.5, 500 mM NaCl and assayed in a 96-well plate at a final concentration of 2 μM in 20 μL volume. Compounds (TPOP146) are added at a final concentration of 10 μM. SYPRO Orange (Molecular Probes) is added as a fluorescence probe at a dilution of 1:1000. Excitation and emission filters for the SYPRO Orange dye are set to 465 and 590 nm, respectively. The temperature is raised with a step of 3°C per minute from 25 to 96°C, and fluorescence readings are taken at each interval^[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]. Popp TA, et al. Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors. J Med Chem. 2016 Oct 13;59(19):8889-8912.

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CBP/p300 ligand 2

发表于2024年2月23日由上海金畔生物科技有限公司

CBP/p300 ligand 2 纯度: 98.17%

CBP/p300 ligand 2 是 dCBP-1 的 PROTAC 靶蛋白的配体。dCBP-1 是一种有效且选择性的 p300/CBP 异双功能降解剂。

CBP/p300 ligand 2 Chemical Structure

CAS No. : 2484741-78-6

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥5770	In-stock
5 mg	￥5000	In-stock
10 mg	￥8500	In-stock
25 mg	￥18000	In-stock
50 mg	￥30000	In-stock
100 mg	￥46000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

CBP/p300 ligand 2 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Anti-Cancer Compound Library

生物活性

CBP/p300 ligand 2 is a ligand for target protein for PROTAC of dCBP-1. dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP^[1].

体外研究
(In Vitro)

CBP/p300 ligand 2 (example 229) has no toxicity to LNCaP prostate cancer 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

524.61

Formula

C₂₇H₃₄F₂N₈O

CAS 号

2484741-78-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据

In Vitro:

DMSO : 200 mg/mL (381.24 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9062 mL	9.5309 mL	19.0618 mL
5 mM	0.3812 mL	1.9062 mL	3.8124 mL
10 mM	0.1906 mL	0.9531 mL	1.9062 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 (9.53 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (9.53 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 (9.53 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (9.53 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

*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]. Jing Liu, et al. Cyclic-amp response element binding protein (cbp) and/or adenoviral e1a binding protein of 300 kda (p300) degradation compounds and methods of use. O2020173440A1.

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CBP/p300-IN-17

发表于2023年12月20日由上海金畔生物科技有限公司

CBP/p300-IN-17

CBP/p300-IN-17 (compound 7) 是一种有效的 EP300/CBP HAT 抑制剂，HAT EP300 和 LK2 H3K27 的 IC₅₀ 分别为0.18, 0.69 µM。

CBP/p300-IN-17 Chemical Structure

CAS No. : 2259640-87-2

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

* Please select Quantity before adding items.

生物活性

CBP/p300-IN-17 (compound 7) is a potent EP300/CBP HAT inhibitor with IC₅₀s of 0.18, 0.69 µM for HAT EP300 and LK2 H3K27, respectively^[1].

IC₅₀ & Target^[1]

EP300

0.18 μM (IC₅₀)

LK2 H3K27

0.69 μM (IC₅₀)

分子量

432.51

Formula

C₂₅H₂₈N₄O₃

CAS 号

2259640-87-2

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]. Kanada R, et al. Discovery of EP300/CBP histone acetyltransferase inhibitors through scaffold hopping of 1,4-oxazepane ring. Bioorg Med Chem Lett. 2022 Jun 15;66:128726.

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CBP/p300-IN-19

发表于2023年12月20日由上海金畔生物科技有限公司

CBP/p300-IN-19

CBP/p300-IN-19 是一种有效的 p300/CBP HAT 抑制剂，p300-HAT, CBP-HAT, PCAF, Myst3 的 IC₅₀s 分别为 1.4, 2.2, >100, > 100 µM。CBP/p300-IN-19 显示出抗肿瘤活性。

CBP/p300-IN-19 Chemical Structure

CAS No. : 2592638-13-4

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

CBP/p300-IN-19 is a potent p300/CBP HAT inhibitor with IC₅₀s of 1.4, 2.2, >100, >100 µM for p300-HAT, CBP-HAT, PCAF, Myst3, respectively. CBP/p300-IN-19 shows antitumor activity^[1].

IC₅₀ & Target^[1]

p300

1.4 μM (IC₅₀)

PCAF

2.2 μM (IC₅₀)

CBP

>100 μM (IC₅₀)

Myst3

>100 μM (IC₅₀)

体外研究
(In Vitro)

CBP/p300-IN-19 (compound 29) shows antiproliferative activity with EC₅₀s of 5.3, 8.5, 6.2, 4.4, 1.2, 4.3, 3.6, 8.7, 6.4 µM for MCF-7, MDA-MB231, LNCaP, PC-3, PANC-1, MDA-PANC-28, Molm-13, MV4;11, RPMI-8226 cells, respectively^[1].
CBP/p300-IN-19 (0, 5, 10 µM; 12 h) dose-dependenly inhibits the acetylation of H3K18, H3K9 and K27^[1].

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

Western Blot Analysis^[1]

Cell Line:	Kasumi-1 leukemia cells
Concentration:	0, 5, 10 µM
Incubation Time:	12 h
Result:	Dose-dependently inhibited the acetylation of H3K18, H3K9 and K27.

分子量

477.55

Formula

C₃₀H₂₇N₃O₃

CAS 号

2592638-13-4

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]. Nie S, et al. Structure-activity relationship and antitumor activity of 1,4-pyrazine-containing inhibitors of histone acetyltransferases P300/CBP. Eur J Med Chem. 2022 Jul 5;237:114407.

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CBP/p300-IN-18

发表于2023年12月20日由上海金畔生物科技有限公司

CBP/p300-IN-18

CBP/p300-IN-18 (compound 8) 是一种有效的 EP300/CBP HAT 抑制剂，HAT EP300 和 LK2 H3K27 的 IC₅₀ 分别为 0.056, 0.46 µM。

CBP/p300-IN-18 Chemical Structure

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生物活性

CBP/p300-IN-18 (compound 8) is a potent EP300/CBP HAT inhibitor with IC₅₀s of 0.056, 0.46 µM for HAT EP300 and LK2 H3K27, respectively^[1].

IC₅₀ & Target^[1]

EP300

0.056 μM (IC₅₀)

LK2 H3K27

0.46 μM (IC₅₀)

分子量

450.51

Formula

C₂₅H₂₇FN₄O₃

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]. Kanada R, et al. Discovery of EP300/CBP histone acetyltransferase inhibitors through scaffold hopping of 1,4-oxazepane ring. Bioorg Med Chem Lett. 2022 Jun 15;66:128726.

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CBP/p300-IN-19 hydrochloride

发表于2023年12月19日由上海金畔生物科技有限公司

CBP/p300-IN-19 hydrochloride

CBP/p300-IN-19 hydrochloride 是一种有效的选择性 p300/CBP HAT 抑制剂，p300-HAT, CBP-HAT, PCAF, Myst3 的 IC₅₀s 分别为 1.4, 2.2, >100, > 100 µM。CBP/p300-IN-19 hydrochloride 显示出抗肿瘤活性

CBP/p300-IN-19 hydrochloride Chemical Structure

CAS No. : 2592638-14-5

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

CBP/p300-IN-19 hydrochloride is a potent and selective p300/CBP HAT inhibitor with IC₅₀s of 1.4, 2.2, >100, >100 µM for p300-HAT, CBP-HAT, PCAF, Myst3, respectively. CBP/p300-IN-19 hydrochloride shows antitumor activity^[1].

IC₅₀ & Target^[1]

p300

1.4 μM (IC₅₀)

PCAF

2.2 μM (IC₅₀)

CBP

>100 μM (IC₅₀)

Myst3

>100 μM (IC₅₀)

体外研究
(In Vitro)

CBP/p300-IN-19 hydrochloride (compound 29) shows antiproliferative activity with EC₅₀s of 5.3, 8.5, 6.2, 4.4, 1.2, 4.3, 3.6, 8.7, 6.4 µM for MCF-7, MDA-MB231, LNCaP, PC-3, PANC-1, MDA-PANC-28, Molm-13, MV4;11, RPMI-8226 cells, respectively^[1].
CBP/p300-IN-19 hydrochloride (0, 5, 10 µM; 12 h) dose-dependenly inhibits the acetylation of H3K18, H3K9 and K27^[1].

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

Western Blot Analysis^[1]

Cell Line:	Kasumi-1 leukemia cells
Concentration:	0, 5, 10 µM
Incubation Time:	12 h
Result:	Dose-dependently inhibited the acetylation of H3K18, H3K9 and K27.

分子量

514.01

Formula

C₃₀H₂₈ClN₃O₃

CAS 号

2592638-14-5

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]. Nie S, et al. Structure-activity relationship and antitumor activity of 1,4-pyrazine-containing inhibitors of histone acetyltransferases P300/CBP. Eur J Med Chem. 2022 Jul 5;237:114407.

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