Potent and selective BRD4 bromodomain inhibitor (Ki = 30 - 50nM for the first bromodomain (BRD4(1)). Exhibits 10-fold selectivity for BRD4(1) over BRD4(2). Blocks BRD4 transcriptional activity in lipopolysaccharide-induced production of both nitric oxide and IL-6 in mouse macrophages (IC50 values are 3.8 and 4.9µM, respectively). Attenuates melanoma cell proliferation in vitro.
Chemical Name: (E)-4-[2-(2-Amino-4-hydroxy-5-methylphenyl)diazenyl]-N-2-pyridinylbenzenesulfonamide
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