PFI-2 ( R)-PFI-2 )

Catalog No. M12414 CAS No. 1627676-59-8

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HPLC

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Product Name

PFI-2
Note

Research use only, not for human use.
Brief Description

A first-in-class, potent and selective inhibitor of SETD7 methyltransferase with Ki app/IC50 of 0.33/2 nM.
Description

A first-in-class, potent and selective inhibitor of SETD7 methyltransferase with Ki app/IC50 of 0.33/2 nM; shows high selectivity (>1,000-fold) for SETD7 over 18 other methyltransferases and DNMT1, 500-fold more active than enantiomer (S)-PFI-2; increases YAP nuclear localization, regulates YAP target genes, and phenocopys the effects of Setd7 deficiency on Hippo pathway signaling in murine embryonic fibroblasts.
Synonyms

R)-PFI-2
Pathway

Chromatin/Epigenetic
Target

HMTase
Recptor

SETD7
Research Area

Other Indications
Indication

——

CAS Number

1627676-59-8
Formula Weight

499.52
Molecular Formula

C23H25F4N3O3S
Purity

>98% (HPLC)
Solubility

10 mM in DMSO
SMILES

C1CCN(C1)C(=O)[C@@H](CC2=CC(=CC=C2)C(F)(F)F)NS(=O)(=O)C3=CC(=C4CNCCC4=C3)F
Chemical Name

6-Isoquinolinesulfonamide, 8-fluoro-1,2,3,4-tetrahydro-N-[(1R)-2-oxo-2-(1-pyrrolidinyl)-1-[[3-(trifluoromethyl)phenyl]methyl]ethyl]-

1. Barsyte-Lovejoy D, et al. Proc Natl Acad Sci U S A. 2014 Sep 2;111(35):12853-8.
2. Niu Y, et al. Sci Rep. 2017 Apr 18;7:46547.

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