(R)-PFI-2 (hydrochloride)

SET domain-containing protein 7/9 (SET7/9) is a histone methyltransferase that monomethylates lysine 4 of histone H3, which generates a specific tag for epigenetic transcriptional activation. It plays a role in the transcriptional activation of tumor suppressor p53 in response to DNA damage as well as the transcription factor TAF10.{16846,17223} (R)-PFI-2 is a potent, cell-permeable inhibitor of SET7/9 (IC50 = 2 nM) that demonstrates greater than 1,000-fold selectivity over a panel of 18 other methyltransferases.{26909} Its enantiomer, (S)-PFI-2 (Item No. 18119), is 500-fold less active (IC50 = 1 µM).{26909} See the Structural Genomics Consortium (SGC) website for more information.