BET bromodomain-IN-5 is an orally active BET inhibitor with an IC50 of 14 nM against BRD4 (1). BET bromodomain-IN-5 can inhibit the proliferation of tumor cells and induce cell cycle arrest and apoptosis. BET bromodomain-IN-5 can be used in the research of tumors [1] [2].
In Vitro, BET bromodomain inhibitor (Compound 11) (0.001-10 μM; 4 days) can inhibit the proliferation of KMS-28PE plasmacytoma cells and AMO-1 multiple myeloma cells, and induce cell cycle arrest and apoptosis[1]. BET bromodomain inhibitor (Compound 44) has a GI50 of 15 nM against MV4-11 cells[2].
References:
[1]. Andrew Ryan CONERY, et al. EXPRESSION LEVELS OF BCL-xL, BCL2, BCL-w, AND BAD AND CANCER THERAPIES. WO2015153871A2. 2015-10-08.
[2]. Romero FA, et al. Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors. J Med Chem. 2016 Feb 25;59(4):1271-98.
In Vitro, BET bromodomain inhibitor (Compound 11) (0.001-10 μM; 4 days) can inhibit the proliferation of KMS-28PE plasmacytoma cells and AMO-1 multiple myeloma cells, and induce cell cycle arrest and apoptosis[1]. BET bromodomain inhibitor (Compound 44) has a GI50 of 15 nM against MV4-11 cells[2].
References:
[1]. Andrew Ryan CONERY, et al. EXPRESSION LEVELS OF BCL-xL, BCL2, BCL-w, AND BAD AND CANCER THERAPIES. WO2015153871A2. 2015-10-08.
[2]. Romero FA, et al. Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors. J Med Chem. 2016 Feb 25;59(4):1271-98.