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Cat.No. 5576 - PFI 4 | C21H24N4O3 | CAS No. 900305-37-5
Description: Potent and selective BRPF1B bromodomain inhibitor
Chemical Name: N-[2,3-Dihydro-1,3-dimethyl-2-oxo-6-(1-pyrrolidinyl)-1H-benzimidazol-5-yl]-2-methoxybenzamide
Purity: ≥99% (HPLC)
Literature (5)

Biological Activity for PFI 4

PFI 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.

Licensing Information

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.

Compound Libraries for PFI 4

PFI 4 is also offered as part of the Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data for PFI 4

M. Wt 380.44
Formula C21H24N4O3
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 900305-37-5
PubChem ID 40642506
Smiles CN(C1=CC(NC(C2=C(OC)C=CC=C2)=O)=C(N3CCCC3)C=C1N4C)C4=O

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.

Solubility Data for PFI 4

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 19.02 50
ethanol 3.8 10

Preparing Stock Solutions for PFI 4

The following data is based on the product molecular weight 380.44. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 5.26 mL 26.29 mL 52.57 mL
2.5 mM 1.05 mL 5.26 mL 10.51 mL
5 mM 0.53 mL 2.63 mL 5.26 mL
25 mM 0.11 mL 0.53 mL 1.05 mL

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References for PFI 4

References are publications that support the biological activity of the product.

Demont et al (2014) 1,3-Dimethyl Benzimidazolones are potent, selective inhibitors of the BRPF1 bromodomain. ACS Med.Chem.Lett. 5 1190 PMID: 25408830

Meier et al (2017) Selective targeting of bromodomains of the bromodomain-PHD fingers family impairs osteoclast differentiation. ACS Chem.Biol. 12 2619 PMID: 28849908

If you know of a relevant reference for PFI 4, please let us know.

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Citations for PFI 4

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Literature in this Area

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