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PFI-2 hydrochloride

Chemical Structure : PFI-2 hydrochloride

CAS No.: 1627607-87-7

PFI-2 hydrochloride ((R)-PFI-2 hydrochloride)

Catalog No.: PC-45489Not For Human Use, Lab Use Only.

PFI-2 ((R)-PFI-2) hydrochloride is a first-in-class, potent and selective inhibitor of SETD7 methyltransferase with Ki app/IC50 of 0.33/2 nM, respectively.

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Biological Activity

PFI-2 ((R)-PFI-2) hydrochloride is a first-in-class, potent and selective inhibitor of SETD7 methyltransferase with Ki app/IC50 of 0.33/2 nM, respectively.
PFI-2 shows high selectivity (>1,000-fold) for SETD7 over 18 other methyltransferases and DNMT1, 500-fold more active than enantiomer (S)-PFI-2.
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.

Physicochemical Properties

M.Wt 535.9825
Formula C23H26ClF4N3O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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Solubility

DMSO: ≥ 32 mg/mL

Chemical Name/SMILES

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

References

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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