Kinase selectivity profile of AS041164 and LY294002
All assays were performed in duplicate at 1 μM compound concentration, and in each case, the kinase activity is expressed as a percentage of that in controls. ATP was 10 μM in all assays. For method details, refer to Camps et al. (2005).
| Kinase | Kinase Activity | Kinase | Kinase Activity (% Control) | ||
|---|---|---|---|---|---|
| AS041164 | LY294002 | AS041164 | LY294002 | ||
| % Control | % Control | ||||
| c-RAF (h) | 104 | 61 | p70S6K (h) | 92 | 90 |
| MEK1 (h) | 104 | 105 | CHK1 (h) | 101 | 105 |
| MKK6 (h) | 104 | 107 | PKBα (h) | 96 | 91 |
| SAPK2a (h) | 103 | 93 | cSRC (h) | 98 | 94 |
| SAPK2b (h) | 91 | 101 | CDK2/cyclinA (h) | 97 | 75 |
| SAPK3 (h) | 81 | 81 | CaMKII (r) | 92 | 97 |
| SAPK4 (h) | 96 | 89 | PRK2 (h) | 112 | 76 |
| MAPKAP-K2 (h) | 107 | 91 | CHK2 (h) | 105 | 97 |
| MSK1 (h) | 94 | 99 | Fyn (h) | 85 | 99 |
| MKK4 (m) | 113 | 86 | JNK3 (r) | 109 | 82 |
| MKK7β (h) | 103 | 113 | CDK1/cyclinB (h) | 81 | 84 |
| JNK1α1 (h) | 108 | 101 | MAPK1 (h) | 95 | 101 |
| JNK2α2 (h) | 107 | 96 | PKCβII (h) | 116 | 101 |
| PDK1 (h) | 103 | 98 | PKCγ (h) | 108 | 98 |
| SGK (h) | 97 | 101 | ZAP-70 (h) | 107 | 81 |
| GSK3β (h) | 97 | 56 | CK1 (y) | 87 | 47 |
| PKA (b) | 97 | 96 | MAPK2 (m) | 100 | 84 |
| PKCα (h) | 101 | 101 | AMPK (r) | 104 | 95 |
| ROCK-II (r) | 103 | 107 | Lck (h) | 108 | 179 |
h, human; r, rat; y, yeast; m, mouse; b, bovine.