BY27 is a potent and selective BET BD2 inhibitor, shows 38, 5, 7, and 21-fold BD1/BD2 selectivity for BRD2, BRD3, BRD4, and BRDT. Anti-cancer activity[1].
BRD2 BD2: 3.1 nM (Ki); BRD2 BD1: 95.5 nM (Ki); BRD3 BD2: 5.3 nM (Ki); BRD3 BD1: 77.9 nM (Ki); BRD4 BD2: 7.3 nM (Ki); BRD4 BD1: 80 nM (Ki); BRD2 BD2: 1.2 nM (Kd); BRD2 BD1: 45 nM (Kd); BRD3 BD2: 2.6 nM (Kd); BRD3 BD1: 12 nM (Kd); BRD4 BD2: 3.5 nM (Kd); BRD4 BD1: 26 nM (Kd); BRDT BD2: 3 nM (Kd); BRDT BD1: 64 nM (Kd)
