PFI-2

PFI-2 is a novel potent and selective SETD7 histone lysine methyltransferase inhibitor (IC₅₀ ~2 nM). It has > 100-fold selectivity over other methyltransferases and other non-epigenetic targets. PFI-2 has been shown to bind to SETD7 by ITC (Kd = 18 nM), and biotinylated PFI-2 interacts with SETD7 in pull-down studies.