Table 2.

Selective disruption of STAT family members by peptidomimetics

MimeticsIC50 Values (μm) against STAT Dimersa
Stat3:Stat3Stat1:Stat3Stat1:Stat1Stat5:Stat5
ISS 22175 ± 36455 ± 97310 ± 7450 ± 12
ISS 49338 ± 16230 ± 22273 ± 22300 ± 23
ISS 59348 ± 3287 ± 15175 ± 6510 ± 6
ISS 61042 ± 23125 ± 15310 ± 145285 ± 32
ISS 63755 ± 35195 ± 12255 ± 55695 ± 123
  • Note: Nuclear extracts containing active Stat1, Stat3, and Stat5 were preincubated with or without peptidomimetics for 30 min before incubation with radiolabeled hSIE probe and EMSA analysis.

  • a Values are the means and SDs of at least three independent assays, ne, no effect at 1 mm.Results are representative peptidomimetics from over 80 that have been evaluated.