Catalog Number: 4892
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 also available.

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.
Additional Information
Licensing Caveats:
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.
Other Product-Specific Information:
Background References
  1. (R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells.
    Barsyte-Lovejoy et al.
    Proc.Natl.Acad.Sci.U S A, 2014;111:12853
Citations:

The citations listed below are publications that use Tocris products. Selected citations for (R)-PFI 2 hydrochloride include:

2 Citations: Showing 1 - 2
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  1. Repression of hypoxia-inducible factor α signaling by Set7-mediated methylation.
    Authors: Liu Et al.
    J Neuroinflammation 2015;43:5081
  2. (R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells.
    Authors: Barsyte-Lovejoy Et al.
    Proc Natl Acad Sci U S A 2014;111:12853
Tocris Small Molecules
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(S)-PFI 2 hydrochloride

5400  
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