(R)-PFI 2 hydrochloride
Potent and selective SETD7 histone lysine methyltransferase inhibitor (IC50 = 2 nM). Exhibits >1000-fold selectivity over DNMT1 and a panel of 18 other methyltransferases. Inhibits YAP nuclear translocation and function following activation of the Hippo signaling pathway in MCF7 cells. Negative control (S)-PFI 2 hydrochloride (Cat. No. 5400) available.
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the (R)-PFI 2 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 (R)-PFI 2 is reviewed on the chemical probes website.
|Storage||Store at -20°C|
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|
|ethanol||10.72||20mM with sonication|
Preparing Stock Solutions
The following data is based on the product molecular weight 535.98. 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||1.87 mL||9.33 mL||18.66 mL|
|5 mM||0.37 mL||1.87 mL||3.73 mL|
|10 mM||0.19 mL||0.93 mL||1.87 mL|
|50 mM||0.04 mL||0.19 mL||0.37 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.
Barsyte-Lovejoy et al (2014) (R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells. Proc.Natl.Acad.Sci.U S A 111 12853 PMID: 25136132
If you know of a relevant reference for (R)-PFI 2 hydrochloride, please let us know.
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1 Citation for (R)-PFI 2 hydrochloride
Citations are publications that use Tocris products. Selected citations for (R)-PFI 2 hydrochloride include:
Liu et al (2015) Repression of hypoxia-inducible factor α signaling by Set7-mediated methylation. J Neuroinflammation 43 5081 PMID: 25897119
Do you know of a great paper that uses (R)-PFI 2 hydrochloride from Tocris? If so please let us know.
Literature in this Area
Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.