Table 2.
Effect of JNK2 Mutations on the Sensitivity of JNK towards (−)-zuonin A.
| Mutants | Kmb μM | kcatb s-1 | kcat/Km μM s-1 | IC50a μM | % Inhibition at 200 μM |
|---|---|---|---|---|---|
| JNK2 WT | 1.65±0.1 | 1±0.15 | 0.6 | 2.9±0.17 | 70% |
| JNK2 (R127A) | 23.6±1.1 | 1.4±0.3 | 0.06 | 14±2.1 | 80% |
| JNK2 (Y130A) | 1.87±0.3 | 1±0.04 | 0.53 | 2.3±0.16 | 95% |
| JNK2 (C163A) | 1.33±0.4 | 1±0.065 | 0.75 | 37±2.5 | 37% |
| JNK2 (T164A) | 0.73±0.18 | 1.1±0.064 | 1.5 | 13.6±1.5 | 39% |
| JNK2 (W324A) | 2.3±0.15 | 1.06±0.075 | 0.46 | 16.6±0.17 | 98% |
| JNK2 (D326A) | 2±0.83 | 0.8±0.08 | 0.4 | 2.8±0.32 | 71% |
IC50 Determined as described in Methods section, Data were fitted to equation 4
Initial velocity data at different concentrations of c-Jun were fitted to equation 1