SETD7/KMT7 Inhibitor

PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride is a potent and selective SET domain containing lysine methyltransferase 7 (SETD7) inhibitor. (R)-PFI-2 shows high inhibiting activity with IC₅₀ value of 2.0  nM and (S)-PFI-2 shows inhibiting activity with IC₅₀  value of 1.0  μM. PFI-2 hydrochloride can be used for the research of chronic kidney disease and inflammation response in the development of renal fibrosis.

PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride, a chemical probe, is a potent and selective SET domain containing lysine methyltransferase 7 (SETD7) inhibitor. (R)-PFI-2 shows high inhibiting activity with IC₅₀ value of 2.0 nM and (S)-PFI-2 shows inhibiting activity with IC₅₀ value of 1.0 μM. PFI-2 hydrochloride can be used for the research of chronic kidney disease and inflammation response in the development of renal fibrosis.

DC-S238 is an orally active and highly selective histone methyltransferase SET7 (SETD7) inhibitor (IC₅₀=4.88 μM). DC-S238 is promising for research of cancer, diabetes and inflammatory diseases.