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Description: GSK5959 is a novel, potent, selective and cell permeable BRPF1 (bromodomain and PHD finger-containing) bromodomain inhibitor with an IC50 of 80 nM. It exhibits > 100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains. The BRPF protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes and are involved in the epigenetic regulation of gene expression and have been implicated in human cancer.
References: ACS Med Chem Lett. 2014 Sep 10; 5(11):1190-5.
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