DCG066 is a novel small molecule inhibitors of lysine methyltransferase G9a, inhibits G9a methyltransferase activity with IC50 of 6.5 uM. DCG066 inhibits cancer cell proliferation, decreases histone H3 lysine 9 (H3K9) di-methyl levels, blocks cell cycle and induces apoptosis. DCG066 (1-2 uM) decreased H3K9-dimethylation in K562 cells, but displayed no changes in H3K27 tri-methylation. DCG066 can bind to G9a with low dissociation constant (Kd = 18 μM) as measured by SPR.
