MS436 - CAS 1395084-25-9
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Not Intended for Therapeutic Use. For research use only.
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BET Bromodomain
MS436 exhibits low nanomolar affinity with preference for the first bromodomain over the second.
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1.Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains.
Zhang G1, Plotnikov AN, Rusinova E, Shen T, Morohashi K, Joshua J, Zeng L, Mujtaba S, Ohlmeyer M, Zhou MM. J Med Chem. 2013 Nov 27;56(22):9251-64. doi: 10.1021/jm401334s. Epub 2013 Nov 11.
BRD4, characterized by two acetyl-lysine binding bromodomains and an extra-terminal (ET) domain, is a key chromatin organizer that directs gene activation in chromatin through transcription factor recruitment, enhancer assembly, and pause release of the RNA polymerase II complex for transcription elongation. BRD4 has been recently validated as a new epigenetic drug target for cancer and inflammation. Our current knowledge of the functional differences of the two bromodomains of BRD4, however, is limited and is hindered by the lack of selective inhibitors. Here, we report our structure-guided development of diazobenzene-based small-molecule inhibitors for the BRD4 bromodomains that have over 90% sequence identity at the acetyl-lysine binding site. Our lead compound, MS436, through a set of water-mediated interactions, exhibits low nanomolar affinity (estimated Ki of 30-50 nM), with preference for the first bromodomain over the second. We demonstrated that MS436 effectively inhibits BRD4 activity in NF-κB-directed production of nitric oxide and proinflammatory cytokine interleukin-6 in murine macrophages.
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CAS 1395084-25-9 MS436

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