MS479 is a BRD4 PROTAC degrader. MS479 binds BRD4-BD2 and GLP with high affinities (BRD4-BD2: Kd = 200 nM, GLP: Kd = 306 nM). MS479 can reduce the protein level of BRD4 short isoform. MS479 recruits the E3 ligase SPOP by directly binding its substrate GLP as a bridge protein. MS479 can be used to inhibit the proliferation of colorectal cancer cells. (Pink: BRD4 ligand (HY-78695), Blue: GLP ligand (HY-176036), Black: linker (HY-176037), GLP ligand+linker: HY-176038)[1].
Molekulargewicht:
1092.87
Formel:
C59H82ClN11O5S
Target-Kategorie:
Epigenetic Reader Domain,PROTACs
Anwendungsbeschreibung:
MCE Product type: Reference compound
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