TABLE 1.
IC50 values for PTP4A3 inhibitors
The in vitro IC50 values for the iminopyridinediones were determined with recombinant human protein using the artificial substrate DiFMUP, an automated liquid handling platform, and 25-minute incubation. N = 3 independent experiments unless otherwise marked.
| Compound | Mean (nM) ± S.E.M. | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| PTP4A1 | PTP4A2 | PTP4A3 | PTP4A3 C49S | PTP4A3 K144I | PTP4A3 A106V | PTP4A3 A111S | CDC25B | DUSP3 | |
| JMS-053 | 29.1 ± 2.7 | 48.0 ± 14.5 | 34.7 ± 2.5a | 156.5 ± 20.1b | 42.7 ± 8.0 | 26.3 ± 2.5 | 104.4 ± 7.7b,c | 92.6 ± 10.2 | 207.6 ± 46.3 |
| EJR-866-81 | 49.0 ± 5.0 | 112.9 ±10.0b | 36.1 ± 1.4 | 390.0 ± 72.5b | 59.1 ± 5.9 | 54.5 ± 2.4 | 61.0 ± 2.8b,c | 65.5 ± 16.6 | 240.8 ± 30.9 |
| EJR-866-75 | 43.2 ± 8.5 | 73.9 ± 10.0 | 98.2 ± 2.5d | 229.7 ±54.6b | 68.5 ± 1.0 | 57.5 ± 18.6 | 172.0 ± 46.0b,c,d | 122.6 ± 22.6 | 521.0 ± 128.4 |
| NRT-870-59e | 133.2 ± 31.7a | 264.4 ± 37.4a,b | 86.0 ± 12.6a | 332.2 ± 52.5b | 180.2 ± 64.5e | 57.7 ± 18.6 | >1000c | >1000 | 411.8 ± 75.3 |
| JMS-038 | >1000 | >1000 | >1000 | ND | >1000 | ND | ND | ND | >1000 |
ND, not determined.
a
N = 8.
b
P < 0.05 compared with PTP4A3.
c
N = 2.
d
N = 6.
e
N = 5.