Table 1.

Disruption of Stat3 DNA-binding activity by peptidomimetics

CompoundR′IC50(μM)a
ProlylphosphotyrosylleucineEmbedded Image182±15
AlanylphosphotyrosylleucineEmbedded Image217±55
ISS 248Embedded Imagene
ISS 265Embedded Imagene
ISS 375Embedded Imagene
ISS 610Embedded Image42±23
ISS 637Embedded Image55±35
ISS 219Embedded Image232±16
ISS 221Embedded Image75±36
ISS 593Embedded Image48±32
ISS 223Embedded Image225±15
ISS 249Embedded Imagene
ISS 493Embedded Image38±16
ISS 352Embedded Image410±15
ISS 353Embedded Image650±22
ISS 355Embedded Imagene
ISS 360Embedded Image420±35
ISS 363Embedded Image643±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).