Chemical Name: N-[2,3-Dihydro-1,3-dimethyl-2-oxo-6-(1-pyrrolidinyl)-1H-benzimidazol-5-yl]-2-methoxybenzamide
Biological ActivityPFI 4 is a potent and selective BRPF1B bromodomain inhibitor (IC50 = 172 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. Inhibits osteoclastogenesis.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Complete Your Research
1,3-dimethyl benzimidazolones are potent, selective inhibitors of the BRPF1 bromodomain.
Demont et al.
ACS Med.Chem.Lett., 2014;5:1190
Selective targeting of bromodomains of the bromodomain-PHD fingers family impairs osteoclast differentiation.
Meier et al.
ACS Chem.Biol., 2017;12:2619
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