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.

CompoundMean (nM) ± S.E.M.
PTP4A1PTP4A2PTP4A3PTP4A3 C49SPTP4A3 K144IPTP4A3 A106VPTP4A3 A111SCDC25BDUSP3
JMS-05329.1 ± 2.748.0 ± 14.534.7 ± 2.5a156.5 ± 20.1b42.7 ± 8.026.3 ± 2.5104.4 ± 7.7b,c92.6 ± 10.2207.6 ± 46.3
EJR-866-8149.0 ± 5.0112.9 ±10.0b36.1 ± 1.4390.0 ± 72.5b59.1 ± 5.954.5 ± 2.461.0 ± 2.8b,c65.5 ± 16.6240.8 ± 30.9
EJR-866-7543.2 ± 8.573.9 ± 10.098.2 ± 2.5d229.7 ±54.6b68.5 ± 1.057.5 ± 18.6172.0 ± 46.0b,c,d122.6 ± 22.6521.0 ± 128.4
NRT-870-59e133.2 ± 31.7a264.4 ± 37.4a,b86.0 ± 12.6a332.2 ± 52.5b180.2 ± 64.5e57.7 ± 18.6>1000c>1000411.8 ± 75.3
JMS-038>1000>1000>1000ND>1000NDNDND>1000
  • ND, not determined.

  • a N = 8.

  • b P < 0.05 compared with PTP4A3.

  • c N = 2.

  • d N = 6.

  • e N = 5.