CPI-637

CPI-637 is a potent and selective CBP/ EP300 bromodomain inhibitor. The biochemical potency of CPI-637 translated well into cells (CBP BRET EC50 = 0.3 μM). CPI-637 demonstrated a >700-fold selectivity over the BET family of bromodomains (BRD4 IC50 = 11.0 ± 0.6 μM). CPI-637 inhibits MYC expression in AMO-1 cells (EC50 = 0.60 μM). CBP and EP300 are highly homologous, bromodomain-containing transcription coactivators involved in numerous cellular pathways relevant to oncology.