SET domain-containing protein 8 (SET8) is a methyltransferase that selectively mono-methylates histone H4 at lysine residue 20, an event proven to have an important role in chromatin structure and transcriptional activation. It is also a regulator of p53, mono-methylating lysine 382 of the tumor suppressor. UNC0379 is a substrate-competitive inhibitor of the lysine methyltransferase SET8 (IC50 = 7.3 ?M; Kd = 18.3 ?M).1 It is selective for SET8 over 15 other methyltransferases, including G9a and GLP (IC50s = >100 ?M).1
1.Ma, A., Yu, W., Li, F., et al.Discovery of a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8J. Med. Chem.(2014)