PFI 4

Pricing Availability Delivery Time Qty
Cat.No. 5576 - PFI 4 | C21H24N4O3 | CAS No. 900305-37-5
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% (HPLC)
Datasheet
Citations
Literature

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.

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

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

Technical Data

M. Wt 380.44
Formula C21H24N4O3
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 900305-37-5
PubChem ID 40642506
InChI Key QCIJLRJBZDBVDB-UHFFFAOYSA-N
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

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

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.63 mL 13.14 mL 26.29 mL
5 mM 0.53 mL 2.63 mL 5.26 mL
10 mM 0.26 mL 1.31 mL 2.63 mL
50 mM 0.05 mL 0.26 mL 0.53 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Keywords: PFI 4, supplier, PFI4, potent, selective, BRPF1, bromodomains, epigenetics, inhibitors, inhibits, sgc, Bromodomains, Bromodomains, Tocris Bioscience

Citations for PFI 4

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