Table 1. JNK inhibitors potency in vitro and in vivo.
Biochemical IC50 in nanomolar for JNK inhibitors against JNK1/2/3 and cellular EC50 for inhibition of c-Jun phosphorylation in Hela and A375 cells. Values for reference inhibitors 5A (Angell et al., 2007), SP-600125 (Bennett et al., 2001) and AS601245 (Gaillard et al., 2005) are from the literature. ND: not determined. See also Table S1.
| IC50 (nM) | p-c-Jun EC50 (nM) | ||||
|---|---|---|---|---|---|
|
|
|||||
| JNK1 | JNK2 | JNK3 | Hela | A375 | |
| JNK-IN-1 | 7780 | 4230 | 7750 | ND | ND |
| JNK-IN-2 | 809 | 1140 | 709 | 704 | 2400 |
| JNK-IN-3 | >10000 | >10000 | >10000 | ND | ND |
| JNK-IN-4 | 2390 | 5460 | 7220 | ND | ND |
| JNK-IN-5 | 2.11 | 1.93 | 0.96 | 118 | 32 |
| JNK-IN-6 | ND | ND | 148 | 6760 | 1905 |
| JNK-IN-7 | 1.54 | 1.99 | 0.75 | 130 | 244 |
| JNK-IN-8 | 4.67 | 18.7 | 0.98 | 486 | 338 |
| JNK-IN-9 | ND | ND | 0.50 | 104 | 117 |
| JNK-IN-10 | ND | ND | 0.50 | 173 | 141 |
| JNK-IN-11 | 1.34 | 0.50 | 0.50 | 48 | 8.6 |
| JNK-IN-12 | 13 | 11.3 | 11.0 | 605 | 134 |
| 5A | 10000* | ND | 200* | >10000 | >10000 |
| SP-600125 | ND | 110* | 190* | 7450 | 1985 |
| AS601245 | 150* | 220* | 70* | 2025 | 2400 |