Chemical Name: N-[2,3-Dihydro-1,3-dimethyl-2-oxo-6-(1-pyrrolidinyl)-1H-benzimidazol-5-yl]-2-methoxybenzamide
Biological ActivityPotent and selective BRPF1 bromodomain inhibitor (IC50 = 80 nM). Exhibits >100-fold selectivity for BRPF1 over a panel of other bromodomains including BRPF2 (BRD1), BRPF3 and BRD4. Disrupts BRPF1 binding to histone H3.3. Cell permeable.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
1,3-dimethyl benzimidazolones are potent, selective inhibitors of the BRPF1 bromodomain.
Demont et al.
ACS Med.Chem.Lett., 2014;5:1190
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