BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. It binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). This inhibitor demonstrates anti-cancer activity.
- Orally active, selective BET bromodomain inhibitor
- High affinity binding to BRD proteins (BRD2(2), BRD3(2), BRD4(1), BRD4(2), BRDT(2))
- Demonstrates anti-cancer activity
- Excellent selectivity for BET bromodomain family
- Does not inhibit five cytochrome P450 enzymes
- Inhibits growth of acute myeloid leukemia and multiple myeloma cell lines
- Exhibits strong antitumor activities in vivo
- Induces G1-phase cell cycle arrest
- Dose-dependent inhibition of c-Myc and upregulation of p21