PFI-2 is a potent inhibitor of SETD7 with IC50 2 nM and 1000-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. Its enantiomer (S)-PFI-2 is 500-fold less active making it an excellent negative control. Treatment of low-density MEFs with (R)-PFI-2 resulted in higher nuclear YAP levels indicating an effect on the Hippo pathway.
Histone Methyltransferase Inhibitors Related Products:
EPZ005687; GSK343; Tazemetostat; UNC1999; MM-102; SGC0946; SGC2085; OICR-9429; HLCL-61 HCL; GSK591; SGC707; GSK503; EPZ015666; UNC0642; UNC0638; GSK-126; EPZ004777; GSK3326595; LLY-507; BRD4770; Pinometostat