STAT3 inhibitor C-188-9

{
  "id": "MLC-T-ONC-016868",
  "term": "STAT3 inhibitor C-188-9",
  "field": "Oncology and biomedicine",
  "definition": "An orally bioavailable, binaphthol-sulfonamide-based inhibitor of signal transducer and activator of transcription 3 (STAT3), with potential antineoplastic activity. Upon oral administration, the STAT3 inhibitor C-188-9 specifically targets and binds to the phosphotyrosyl peptide binding site within the Src homology 2 (SH2) domain of STAT3. This inhibits the Janus kinase (JAK)-mediated tyrosine phosphorylation and activation of STAT3. This impedes nuclear translocation of STAT3, prevents STAT3 binding to responsive gene promoters and blocks STAT3-mediated regulation of gene expression. STAT3 regulates the transcription of genes involved in several cellular functions. STAT3 is constitutively activated in a variety of human cancers and plays a key role in neoplastic transformation, uncontrolled tumor cell proliferation, resistance to apoptosis, metastasis, immune evasion, tumor angiogenesis, epithelial-mesenchymal transition (EMT) and the Warburg effect.",
  "synonyms": [
    "STAT3 inhibitor XIII",
    "STAT3 inhibitor TTI-101"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/stat3-inhibitor-c-188-9/"
}