Description
A fungal mycotoxin that inhibits the histone lysine methyltransferase (HKMT) SU(VAR)3-9 (IC50 = 0.8 µM). Inhibits other Lys9-specific HMTs, including G9a (IC50 = 2.5 µM) and DIM5 (IC50 = 3 µM). Selectivity for Lys9-HMTs is indicated by higher IC50 values (>90 µM) for Lys20-specific PRSET7, Lys27-specific EZH2, and Lys4-specific SET7/9.
Chemical Name
(3S,3'S,5aR,5aR,10bR,10'bR,11aS,11'aS)-2,2',3,3',5a,5'a,6,6'-octahydro-3,3'-bis(hydroxymethyl)-2,2'-dimethyl-[10b,10'b(11H,11'H)-bi3,11a-epidithio-11aH-pyrazino[1',2':1,5]pyrrolo[2,3-b]indole]-1,1',4,4'-tetrone