Potent and selective BRPF1 bromodomain inhibitor (IC50
= 80 nM). Exhibits >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains. Inhibits BRPF1 interaction with histone H3.3. Cell permeable.
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1,3-dimethyl benzimidazolones are potent, selective inhibitors of the BRPF1 bromodomain.
Demont et al.
ACS Med.Chem.Lett., 2014;5:1190