Biological Activity:PFI-2 is a novel potent and selective SETD7 histone lysine methyltransferase inhibitor with 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=18nM), and biotinylated PFI-2 interacts with SETD7 in pull-down studies.
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