Catalog Number: 5576
Chemical Name: N-[2,3-Dihydro-1,3-dimethyl-2-oxo-6-(1-pyrrolidinyl)-1H-benzimidazol-5-yl]-2-methoxybenzamide
Biological Activity
Potent 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.
Technical Data
  • M.Wt:
    380.44
  • Formula:
    C21H24N4O3
  • Solubility:
    Soluble to 50 mM in DMSO and to 10 mM in ethanol
  • Purity:
    >99%
  • Storage:
    Store at +4°C
  • CAS No:
    900305-37-5
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.
Additional Information
Licensing Caveats:
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the PFI 4 probe summary on the SGC website.
Background References
  1. 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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