GNE-272 (GNE272) potent and selective the bromodomains of CBP/EP300 inhibitor with IC50 of 0.02 and 0.03 uM for CBP and EP300, respectively.
GNE-272 displays high selectivity over BRD4 (1) and other BRDs (>10 uM).
GNE-272 shows antiproliferative effect in hematologic cancer cell lines and modulates MYC expression in vivo.
GNE-272 exhibits excellent in vivo PK and antitumor activity in an AML tumor model.
