Table 4.
Selectivity studies of STEP inhibitors with a panel of protein phosphatases.
| PTPs | Inhibitory activity (μM) |
|||
|---|---|---|---|---|
| ST2 | ST2–5 | ST3 | ST3–5 | |
| STEP | 9.7±2.6 | 7.7±1.5 | 10.7±0.9 | 7.5±1.2 |
| VHR | 56.9±9.6 | 26.0±5.0 | 9.1±1.1 | 147.3±25.0 |
| LYP | 33.5±6.1 | 14.5±2.7 | 10.4±2.5 | 19.8±6.4 |
| PTP1B | 13.3±3.9 | 67.6±3.3 | 15.0±5.5 | 12.3±2.3 |
| HePTP | 48.2±11.3 | 20.1±4.0 | 28.7±3.0 | 39.8±4.7 |
| YopH | 26.2±4.4 | 15.3±2.3 | 108.5±25.0 | 333.0±33.6 |
| PP1 | 33.0±4.9 | 32.5±3.3 | 131.1±38.0 | 87.8±21.8 |
| PPM1B | 165.0±21.5 | 191.6±28.6 | 152.8±18.4 | 223.0±10.3 |
| PPM1G | 138.5±23.0 | 188.8±22.7 | 166.9±23.3 | 98.7±21.5 |
| Gleep | 18.3±2.9 | 41.9±6.4 | 213.9±2.0 | 32.3±2.0 |
| PRL | 195.6±21.5 | 288.3±12.3 | >500 | 282.5±9.3 |
a
The data presented are the average of at least three independent measurements. Data were fitted to the Michaelis-Menten equation using nonlinear least squares regression (GraphPad Prism).