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(R)-PFI 2 hydrochloride

Catalog #: 4892
3 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
4892/10
(R)-PFI 2 hydrochloride | CAS No. 1627607-87-7 | Lysine Methyltransferase Inhibitors
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Description: Potent and selective SETD7 inhibitor

Chemical Name: 8-Fluoro-1,2,3,4-tetrahydro-N-[(1R)-2-oxo-2-(1-pyrrolidinyl)-1-[[3-(trifluoromethyl)phenyl]methyl]ethyl]-6-isoquinolinesulfonamide hydrochloride

Purity: ≥97%

Product Details
Citations (3)
Supplemental Products
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

(R)-PFI 2 hydrochloride is a 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Complete Your Experiment

(S)-PFI 2 hydrochloride
Cat # 5400

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. A chemical biology toolbox to study protein methyltransferases and epigenetic signaling.
    Scheer et al.
    Nat.Commun., 2019;10:19
  2. (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

Product Datasheets

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Citations for (R)-PFI 2 hydrochloride

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

3 Citations: Showing 1 - 3

  1. Inhibition of methyltransferase Setd7 allows in vitro expansion of myogenic stem cells with improved therapetic potential.
    Authors: Judson Et al.
    Cell Stem Cell  2018;22:177
  2. Repression of hypoxia-inducible factor α signaling by Set7-mediated methylation.
    Authors: Liu Et al.
    J Neuroinflammation  2015;43:5081
  3. (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

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(S)-PFI 2 hydrochloride

5400
1 Citations
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