BI 894999 (Amredobresib) is a novel potent, selective BET inhibitor with IC50 of 5 and 41 nM for BRD4-BD1 and BRD4-BD2 bromodomains, respectively.
BI 894999 displays excellent selectivity over other bromodomains.
BI 894999 decreases S-Phase and increases apoptosis, Volasertib augments and prolongs the decrease of MYC expression caused by BI 894999 treatment in AML cell lines。
BI 894999 dramatically reduces tumor burden accompanied by eradication of AML cells in mouse bone marrow combined with Volasertib.
BI 894999 also represses super-enhancer-associated transcription and synergizes with CDK9 inhibition in AML.
