Table 1.
IC50 values, or percentage of inhibition at 200 μM, of MC4040 and MC4041 against a panel of methyltransferases
Compound | IC50, μMa or % inhibition at 200 μM | ||||
---|---|---|---|---|---|
EZH2 | EZH1 | G9a | PRMT1 | DNMT1 | |
MC4040 | 4.06 | 42.7 | NAb | NA | NA |
MC4041 | 1.06 | 10.6 | NA | 11.9% | NA |
SAH | 34.7 | ||||
GSK126 | 0.009 | ||||
TAZc | <0.005 |
aPerformed in a 10-dose IC50 mode with 2-fold serial dilution starting from 200 μM. bNA, not active. cTAZ, tazemetostat