GSK-6853

GSK-6853 is a potent and selective BRPF1 inhibitor. GSK-6853 exhibits >1600-fold selectivity for BRPF1 over other bromodomains (pIC50values by TR-FRET are 8.1,5.1/4.8 and 4.7/<4.3 for BRPF1, BRPF2/3 and BRD4 BD1/2, respectively) . The structural analog of GSK-6853, GSK-9311, serves as a good inactive control (125- and 185-fold reduced potency in cell-free and cell-based assays, respectively) .