MS645 is a cell penetrant bivalent bromodomain (BRD) inhibitor that inhibits the tandem BD1/BD2 of BRD4. It potently represses BRD4 transcriptional activity in solid-tumor cells including TNBC. MS645 potently inhibits IL-6 expression MDA-MB-231 cells. MS645 exhibits sustained blockade of BRD4 by inhibition of BRD4 interactions with transcription enhancer/mediator proteins MED1 and YY1.
cell penetrant bivalent bromodomain (BRD) inhibitor that inhibits the tandem BD1/BD2 of BRD4
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11 - Combustible Solids
Classe de risco de água (WGK)
WGK 3
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Not applicable
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Not applicable
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Proceedings of the National Academy of Sciences of the United States of America, 115(31), 7949-7954 (2018-07-18)
The importance of BET protein BRD4 in gene transcription is well recognized through the study of chemical modulation of its characteristic tandem bromodomain (BrD) binding to lysine-acetylated histones and transcription factors. However, while monovalent inhibition of BRD4 by BET BrD
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