Table 1.
Kinase selectivity of 1 and staurosporine
| IC50 ± STDEV (nM) | IC50 ± STDEV (nM) | ||||
|---|---|---|---|---|---|
| 1 (n = 3) | Staurosporine (n = 2) | 1 (n = 3) | Staurosporine (n = 2) | ||
| CDK1/Cyclin A2 | 950 ± 160 | 3 ± 1 | FGFR1 | 8,000 ± 5,000 | <1 |
| CDK2/Cyclin E1 | 160 ± 20 | 43 ± 6 | JAK3 | >50,000 | <1 |
| CDK3/Cyclin E1 | 370 ± 150 | 37 ± 2 | LCK | 30,000 ± 10,000 | 8 ± 3 |
| CDK5/p35 | 260 ± 160 | <1 | SYK | 12,000 ± 3,000 | <1 |
| CDK6/Cyclin D3 | 720 ± 180* | 150 ± 40* | MINK1 | >50,000 | 6.0 ± 1 |
| CDK9/Cyclin K | 19,000 ± 3,000 | 20 ± 7 | PAK1/CDC42 | >50,000 | 60 ± 30* |
| CLK3 | 2,900 ± 400 | 1,200 ± 100 | IRAK4 | >50,000 | 15 ± 7 |
| Aurora A | 13,000 ± 3,000 | 11 ± 4 | TAK1-TAB1 | 17,000 ± 4,000 | 8 ± 1 |
| CK2α1 | 4,000 ± 1,000 | >20,000 | GSK3β | 1,100 ± 200 | 8 ± 2 |
| IKKβ | >50,000 | >20,000 | p38α | >50,000 | >20,000 |
| CK1α1 | 1,200 ± 200 | >20,000 | AMPK α1/β1/γ2 | 100 ± 15 | <1 |
| CK1γ1 | >50,000 | >20,000 | CAMK4 | 600 ± 200 | 21 ± 2 |
| PKCα | >50,000 | <1 | CHK1 | >50,000 | 5 ± 1 |
| ROCK1 | 23,000 ± 4,000 | 4 ± 1 | DAPK1 | >50,000 | 98 ± 7 |
| AKT1 | 6,000 ± 3,000 | 18 ± 7 | MAPKAPK2 | >50,000 | 160 ± 30 |
IC50 values represent the averages from the indicated number of experiments ± SD of the mean. Asterisk denotes enzymes where <70% maximal inhibition was observed.