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.