TABLE 1.
IC50 values and inhibition efficiencies of SHIP2 inhibitors identified in the virtual screening and their specificity for SHIP2 in relation to SHIP1 and PTEN
| Molecule | SHIP2 | SHIP1 | PTEN | |||
|---|---|---|---|---|---|---|
| IC50 (µM) | Inhibition efficiency (%) | IC50 (µM) | Inhibition efficiency (%) | IC50 (µM) | Inhibition efficiency (%) | |
| Metformin | 6.0 | 39.4 | >50 | 11.1 | >50 | 0 |
| Megestrol acetate | 6.2 | 76.6 | 24.6 | 30 | N/T | N/T |
| Mercaptopurine | 8.8 | 52.9 | 21.2 | 11.4 | N/T | N/T |
| Thioguanine | 9 | 44.9 | >50 | 29.9 | N/T | N/T |
| AS1949490 | N/A | 25.9 | >50 | 11.8 | >50 | 0 |
Inhibition efficiencies were determined using the inhibitors at 100 µM concentration. The measurements for SHIP2 and SHIP1 purified His-tagged phosphatase domains were carried out in the High Throughput Biomedicine Unit. N/A, not applicable; N/T, not tested.