PFI-2 hydrochloride

Research use only, not for human use.

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

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.

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Animal Model:Male C57BL/6 mice (8-10-week old, 20-25 g)Dosage:200 μM (PFI-2 is diluted in 100 μL 0.1% (v/v) DMSO to a concentration of 200 μM/100 μL)Administration:intraperitoneal injection, twice a week Result:Presented less bone marrow-derived myofibroblasts, fewer CD206+/α-smooth muscle actin + cells and developed less renal fibrosis (P<0.01). Reduced the infiltration of inflammatory cells and decreased the production of pro-inflammatory cytokines and chemokines in the kidneys after folic acid treatment (P<0.01).Suppressed the accumulation of NF-κB p65+ cells in folic acid nephropathy (P<0.01).

R)-PFI-2 hydrochloride

Chromatin/Epigenetic

HMTase

SETD7

Other Indications

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1627607-87-7

535.9825

C23H26ClF4N3O3S

>98% (HPLC)

DMSO: ≥ 32 mg/mL

C1CCN(C1)C(=O)C(CC2=CC(=CC=C2)C(F)(F)F)NS(=O)(=O)C3=CC4=C(CNCC4)C(=C3)F.Cl

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)

(-20℃)

With Ice Pack

≥ 2 years