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Description: PFI-2 (PFI2) is a novel, potent and selective inhibitor of lysine methyltransferase SETD7 SET domain containing (lysine methyltransferase) 7 with anticancer activity. It inhibits SETD7 with a Ki (app) and IC50 of 0.33 nM and 2 nM, respectively, and shows > 1000-fold selectivity for SETD7 over other methyltransferases and other non-epigenetic targets. In HEK293 cells, (R)-PFI-2 (10 uM) bound to and stabilized SETD7. In Setd7+/+ murine embryonic fibroblasts (MEFs), (R)-PFI-2 increased nuclear localization of Yes-associated protein (YAP) and the expression of YAP target genes Ctgf, Gli2 and Cdc20.
References: Proc Natl Acad Sci U S A. 2014 Sep 2; 111(35):12853-8.
Related CAS #: 1627676-59-8 (free base); 1627607-87-7 (HCl)
Chemical Name: (R)-8-fluoro-N-(1-oxo-1-(pyrrolidin-1-yl)-3-(3-(trifluoromethyl)phenyl)propan-2-yl)-1, 2, 3, 4-tetrahydroisoquinoline-6-sulfonamide hydrochloride
InChi Key: ZADKZNVAJGEFLC-ZMBIFBSDSA-N
InChi Code: InChI=1S/C23H25F4N3O3S.ClH/c24-20-13-18(12-16-6-7-28-14-19(16)20)34(32, 33)29-21(22(31)30-8-1-2-9-30)11-15-4-3-5-17(10-15)23(25, 26)27; /h3-5, 10, 12-13, 21, 28-29H, 1-2, 6-9, 11, 14H2; 1H/t21-; /m1./s1
SMILES Code: O=S(C1=CC2=C(CNCC2)C(F)=C1)(N[CH](CC3=CC=CC(C(F)(F)F)=C3)C(N4CCCC4)=O)=O.[H]Cl
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