Table 3.
Selectivity of compounds towards PRL-3 over other phosphatases. DiFMUP dephosphorylation was measured at the respective KM of each enzyme, at a compound concentration of 50 μM (thienopyridone: 0.5 μM) and enzyme concentration of 35 nM. Selectivity index = 1 – (inhibition of PRL-3/inhibition of enzyme). The closer the value is to 1, the higher the selectivity towards PRL-3.
| Compound | Selectivity index towards PRL-3 over |
||
|---|---|---|---|
| PTP1B | TCPTP | VHR | |
| Thienopyridone | 0.93 | 0.93 | 0.93 |
| Rhodanine control | 0.34 | 0.22 | 0.54 |
| 1 | 0.38 | 0.46 | 0.64 |
| 2 | 0.25 | 0.10 | 0.25 |
| 3 | 0.65 | 0.77 | 0.85 |
| 4 | 0.08 | −0.29 | 0.24 |
| 5 | 0.48 | 0.24 | 0.44 |