CBP/p300-IN-12

发表于由

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。

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

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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