Selective disruption of STAT family members by peptidomimetics
| Mimetics | IC50 Values (μm) against STAT Dimersa | ||||||
|---|---|---|---|---|---|---|---|
| Stat3:Stat3 | Stat1:Stat3 | Stat1:Stat1 | Stat5:Stat5 | ||||
| ISS 221 | 75 ± 36 | 455 ± 97 | 310 ± 74 | 50 ± 12 | |||
| ISS 493 | 38 ± 16 | 230 ± 22 | 273 ± 22 | 300 ± 23 | |||
| ISS 593 | 48 ± 32 | 87 ± 15 | 175 ± 65 | 10 ± 6 | |||
| ISS 610 | 42 ± 23 | 125 ± 15 | 310 ± 145 | 285 ± 32 | |||
| ISS 637 | 55 ± 35 | 195 ± 12 | 255 ± 55 | 695 ± 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.