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(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 also 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|ethanol||10.72||20 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 the degree 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|
References are publications that support the biological activity of the product.
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
Scheer et al (2019) A chemical biology toolbox to study protein methyltransferases and epigenetic signaling. Nat.Commun. 10 19 PMID: 30604761
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2 Citations 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
Judson et al (2018) Inhibition of methyltransferase Setd7 allows in vitro expansion of myogenic stem cells with improved therapetic potential. Cell Stem Cell 22 177 PMID: 29395054
Do you know of a great paper that uses (R)-PFI 2 hydrochloride from Tocris? Please let us know.
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