MS 436 CAS:1395084-25-9 is a potent and selective BRD4 bromodomain inhibitor (Ki of the first bromodomain (BRD4(1)) = 30 – 50 nM), MS436 exhibits in a panel of water-mediated interactions Low nanomolar affinity (estimated Ki is 30-50 nM), with 10-fold selectivity for BRD4(1) over BRD4(2). Blocks BRD4 transcriptional activity in lipopolysaccharide-induced nitric oxide and IL-6 production in mouse macrophages (IC50 values of 3.8 and 4.9 μM, respectively). Attenuates melanoma cell proliferation in vitro. MS436 represents a new class of bromodomain inhibitors that will facilitate further studies on the biological functions of the two bromodomains of BRD4 in gene expression.
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