PFI-2 hydrochloride

  • Chemical Properties
CAS No. 1627607-87-7 Cat. No. BCP19500
Name PFI-2 hydrochloride
Synonyms PFI 2 hydrochloride;PFI2 hydrochloride;
Formula C23H26ClF4N3O3S M. Wt 535.98
  • Biological Activity
Description (R)-PFI-2 is highly selective (>1,000-fold) for SETD7, over a panel of 18 other human protein methyltransferases and DNMT1, and was shown to be inactive against 134 additional ion channel, GPCR, and enzyme targets (<35% inhibition at 10 μM). (R)-PFI-2 binds to SETD7 only in the presence of SAM. PFI-766, a biotinylated variant of (R)-PFI-2 that retains the ability to bind and inhibit SETD7 (IC50 110 ± 26 nM in our in vitro enzymatic assay). PFI-766 engagement of endogenous SETD7 was also confirmed by mass spectrometry that supported the high specificity of the compound for endogenous SETD7.
Pathways Epigenetics 
Targets Histone Methyltransferase 

Structure

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