组蛋白乙酰转移酶抑制剂;Histone Acetyltransferase Inhibitors;;InformationCPI-637 CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor with IC50 values of 0.03 μM and 0.051μM for CBP and EP300 respectively in TR-FRET assay. It is highly selective against other bromodomains, displaying substantial biochemical activity only against BRD9.TargetsCBP (Cell-free assay); EP300 (Cell-free assay) 0.03 μM; 0.051 μMIn vitroCPI-637 inhibits MYC expression in AMO-1 cells (EC50=0.60 μM).Cell Research(from reference)Cell lines:AMO-1 cells Concentrations:0-5 μM Incubation Time:6 h
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.