Table 4.
Comparative inhibition of GSK-3 short from various species, mutants of LmajGSK-3 short, and HsGSK-3β. Displayed are the mean IC50s (μM) and standard deviation of the mean in parentheses.
| Inhibitors: Mean IC50 in μM (SD) | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Enzyme | GW8510 | GSK-3β Inhibitor VIII | TrkA Inhibitor | Angio-genesis inhibitor | Ro-31-7549 | Indirubin-3'-monoxime-5-sulphonic Acid | JAK3 Inhibitor VI | Alster-paullone, 2-cyanoethyl | SU9516 | Cdk1/2 Inhibitor III | Hymeni-aldisine, Stylissa dami-cornis |
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| LinfGSK-3 | 0.63 (0.04) | no activity | no activity | 13.59 (0.89) | 1.52 (0.20) | 2.22 (0.07) | 4.04 (2.49) | 1.04 (0.40) | 1.87 (0.09) | 0.26 (0.09) | 18.25 (3.83) |
| LmajGSK-3 | 0.84 (0.15) | no activity | no activity | 18.30 (0.68) | 1.63 (0.66) | 2.84 (1.01) | 6.79 (0.07) | 1.00 (0.22) | 3.04 (0.24) | 0.32 (0.09) | 13.13 (4.51) |
| LmajEGSK-3 | 0.33 (0.04) | no activity | no activity | 18.02 (2.77) | 1.55 (0.46) | 8.63 (0.88) | 5.82 (0.92) | 4.76 (1.97) | 3.15 (0.29) | 0.46 (0.15) | 10.42 (0.07) |
| LmajFGSK-3 | 0.09 (0.01) | no activity | 16.43 (5.84) | 8.47 (0.38) | 1.08 (0.07) | 0.93 (0.15) | 2.43 (0.05) | 0.31 (0.04) | 1.40 (0.35) | 0.15 (0.05) | 16.07 (2.77) |
| LmajEFGSK-3 | 0.03 (0.01) | 13.31 (1.08) | 6.15 (2.48) | 6.76 (0.74) | 0.89 (0.17) | 2.29 (0.37) | 6.22 (2.62) | 0.87 (0.29) | 1.29 (0.27) | 0.18 (0.06) | 9.25 (0.55) |
| TbruGSK-3 | 0.02 (0.01) | 4.30 (0.90) | 2.81 (0.03) | 2.44 (0.47) | 1.34 (0.48) | 0.48 (0.02) | 1.70 (0.48) | 1.05 (0.29) | 0.59 (0.09) | 0.12 (0.04) | 3.95 (0.47) |
| HsGSK-3b | 0.02 (0.01) | 0.80 (0.16) | 13.93 (2.57) | 1.62 (0.20) | 0.004 (0.001) | 0.06 (0.01) | 1.16 (0.37) | 0.02 (0.01) | 0.41 (0.14) | 0.21 (0.05) | 0.10 (0.02) |