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Chemical Structure : PFI-2
CAS No.: 1627676-59-8
Catalog No.: PC-45488Not For Human Use, Lab Use Only.
PFI-2 ((R)-PFI-2) 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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PFI-2 ((R)-PFI-2) 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.
| M.Wt | 499.5215 | |
| Formula | C23H25F4N3O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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]- |
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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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