MS436

MS436 is a potent and selective BRD4 bromodomain inhibitor (Ki = 30 - 50 nM for BrD1). MS436 effectively inhibits BRD4 activity in NF-κB-directed production of nitric oxide and proinflammatory cytokine interleukin-6 in murine macrophages. MS436 exhibits 10-fold selectivity for BrD1 over BrD2. MS436 blocks BRD4 transcriptional activity in lipopolysaccharide-induced production of both nitric oxide and IL-6 in mouse macrophages (IC50 values are 3.8 and 4.9 μM, respectively).