BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor. It demonstrates high affinity binding to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) and exhibits potent anti-cancer activity.
- Orally active, selective BET bromodomain inhibitor
- IC50 of 2.6 nM for BRD4
- Binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities
- Exhibits potent anti-cancer activity
- Induces G1-phase cell cycle arrest
- Inhibits c-Myc expression and upregulates p21 levels
- Reduces c-Myc, BCL-2, and CDK6 expressions
- Highly selective for BET bromodomain family (~1500-fold over EP300)
- Strong antitumor activities in MV4-11 mouse xenograft model