(R)-PFI 2 hydrochloride

Cat. No. 4892

(R)-PFI 2 hydrochloride C23H25F4N3O3S.HCl [1627607-87-7]

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Chemical Name: (1R)-1-[[3-(Trifluoromethyl)phenyl]methyl]-2-oxo-2-(1-pyrrolidinyl)ethyl]1,2,3,4-tetrahydro-6-isoquinolinesulfonamide hydrochloride

Biological Activity

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.

Licensing Information

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.

Technical Data

M.Wt:
535.98
Formula:
C23H25F4N3O3S.HCl
Solubility:
Soluble to 100 mM in DMSO and to 20 mM in ethanol with sonication
Purity:
>97 %
Storage:
Store at -20°C
CAS No:
1627607-87-7

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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

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 this product please let us know.

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.

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.

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Keywords: (R)-PFI 2 hydrochloride, supplier, (R)-PFI2, HCl, potent, selective, inhibitors, inhibits, SETD7, lysine, histone, methyltransferase, epigenetics, Hippo, YAP, sgc, Tocris Bioscience, Lysine Methyltransferase Inhibitor products

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