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。
货号:ajcx38118
CAS:2738688-57-6
分子式:C33H29F4N5O6
分子量：667.61
溶解度:DMSO : 250 mg/mL (374.47 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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).

[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.