PFI 1

Key Product Details

Product Description

PFI 1 is a potent BET bromodomain inhibitor; exhibits inhibitory activity at bromodomain-containing protein (BRD) 2 and BRD4 (IC₅₀ values are 98 and 220 nM respectively). Induces apoptosis and G₁ cell cycle arrest in BET inhibitor-sensitive cell lines (MV4;11). Also downregulates Aurora B expression in MV4;11 cells. Cell permeable.

Licensing Information

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the PFI 1 probe summary on the SGC website.

External Portal Information

Chemicalprobes.org

is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of PFI 1 is reviewed on the chemical probes website.

Product Specifications for PFI 1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for PFI 1

The following data is based on the product molecular weight 347.39.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

1 Recalculate

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.5 mM	5.76 mL	28.79 mL	57.57 mL
2.5 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.58 mL	2.88 mL	5.76 mL
25 mM	0.12 mL	0.58 mL	1.15 mL

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 6 publications citing the usage of this product.

• Picaud PFI-1 - a highly selective protein interaction inhibitor targeting BET bromodomains. Cancer Res. 2013 PMID: 23576556
• Fish Identification of a chemical probe for bromo and extra c-terminal bromodomain inhibition through optimization of a fragment-derived hit. J.Med.Chem. 2012 PMID: 23095041

Product Documents for PFI 1