PFI 4

Catalog # Availability Size / Price Qty
5576/10
5576/50
Cat.No. 5576 - PFI 4 | C21H24N4O3 | CAS No. 900305-37-5
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Description: Potent and selective BRPF1 bromodomain inhibitor

Chemical Name: N-[2,3-Dihydro-1,3-dimethyl-2-oxo-6-(1-pyrrolidinyl)-1H-benzimidazol-5-yl]-2-methoxybenzamide

Purity: ≥99%

Product Details
Reviews

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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