Table 1.
Inhibition of SMYD3 methylation activity by diperodon in the form of racemic mixture, isolated enantiomers and reconstituted racemic mixture. The reference inhibitor EPZ031686 was used at a concentration close to its IC50 value (0.7 μM [20] ). Values are presented as averages with a corresponding standard deviation.
|
Compound |
Concentration [μM] |
Inhibition [%] |
|---|---|---|
|
rac‐diperodon |
100 |
44.5±2.0 |
|
(S)‐diperodon |
100 |
45.8±1.5 |
|
(R)‐diperodon |
100 |
40.4±1.1 |
|
reconstituted rac‐diperodon |
100 |
39.7±1.6 |
|
EPZ031686 |
0.63 |
52.8±1.7 |