Disruption of Stat3 DNA-binding activity by peptidomimetics
Compound | R′ | IC50(μM)a |
---|---|---|
Prolylphosphotyrosylleucine | ![]() | 182±15 |
Alanylphosphotyrosylleucine | ![]() | 217±55 |
ISS 248 | ![]() | ne |
ISS 265 | ![]() | ne |
ISS 375 | ![]() | ne |
ISS 610 | ![]() | 42±23 |
ISS 637 | ![]() | 55±35 |
ISS 219 | ![]() | 232±16 |
ISS 221 | ![]() | 75±36 |
ISS 593 | ![]() | 48±32 |
ISS 223 | ![]() | 225±15 |
ISS 249 | ![]() | ne |
ISS 493 | ![]() | 38±16 |
ISS 352 | ![]() | 410±15 |
ISS 353 | ![]() | 650±22 |
ISS 355 | ![]() | ne |
ISS 360 | ![]() | 420±35 |
ISS 363 | ![]() | 643±43 |
Note: Nuclear extracts containing active Stat3 were preincubated for 30 min with or without peptidomimetics before incubation with radiolabeled hSIE probe and analysis by EMSA.
↵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. Structural formula of compounds: R′Y*L (where R′ is defined as shown).