Preferred Label : STAT3 Inhibitor C-188-9;
NCIt synonyms : STAT3 Inhibitor XIII; STAT3 Inhibitor TTI-101;
NCIt related terms : TTI-101;
NCIt 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.;
UNII : KZ3DLD11RQ;
InChIKey : QDCJDYWGYVPBDO-UHFFFAOYSA-N;
CAS number : 432001-19-9;
Molecule name : TTI 101; C188-9; TTI-101;
NCI Metathesaurus CUI : CL553271;
Origin ID : C151932;
UMLS CUI : C4548584;
Automatic exact mappings (from CISMeF team)
- Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
- has_target
