CBP/p300-IN-12 is a potent and selective covalent histone acetyltransferases p300 (IC 50 of 166 nM) and CBP inhibitor. CBP/p300-IN-12 decreases the levels of H3K27Ac of PC-3 cells (EC 50 of 37 nM). CBP/p300-IN-12 forms a covalent adduct with C1450.
性状
Solid
IC50 & Target[1][2]
IC50: 166 nM (p300 HAT domain)
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). has not independently confirmed the accuracy of these methods. They are for reference only.
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
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.
溶解度数据
In Vitro: DMSO : 250 mg/mL (374.47 mM; Need ultrasonic)配制储备液