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.
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.
|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 347.39. 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||2.88 mL||14.39 mL||28.79 mL|
|5 mM||0.58 mL||2.88 mL||5.76 mL|
|10 mM||0.29 mL||1.44 mL||2.88 mL|
|50 mM||0.06 mL||0.29 mL||0.58 mL|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
References are publications that support the products' biological activity.
Fish et al (2012) Identification of a chemical probe for bromo and extra c-terminal bromodomain inhibition through optimization of a fragment-derived hit. J.Med.Chem. [Epub ahead of print] PMID: 23095041
If you know of a relevant reference for PFI 1, please let us know.
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Keywords: PFI 1, supplier, PFI1, bet, bromodomain, brd4, brd2, inhibitors, inhibits, epigenetics, atypical, kinases, bromodomain-containing, 2, bromodomain-containing, 4, sgc, Bromodomains, Tocris Bioscience
Citations for PFI 1
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