Preferred Label : Tegavivint;
NCIt synonyms : 9,10-Anthracenedione, 2,7-bis(((3R,5S)-3,5-dimethyl-1-piperidinyl)sulfonyl)-, 9,10-dioxime,
rel-; Tegatrabetan;
NCIt definition : A small molecule inhibitor of the Wnt/beta-catenin pathway with potential antineoplastic
activity. Upon intravenous administration, tegavivint binds to transducin beta-like
protein 1 (TBL1) and disrupts the binding of beta-catenin to TBL1. This promotes beta-catenin
degradation, attenuates nuclear and cytoplasmic levels of beta-catenin, and reduces
transcriptional activity of transcription factor 4 (TCF4) and expression of its target
genes, cyclin D1, c-Myc and survivin. The Wnt/beta-catenin signaling pathway regulates
cell morphology, motility, and proliferation; aberrant regulation of this pathway
leads to neoplastic proliferation. Beta-catenin is frequently mutated in various tumors.;
UNII : 18AP231HUP;
InChIKey : GAPRVZKWPDRAJA-QOPKLXIQSA-N;
CAS number : 1227637-23-1;
Molecule name : BC-2059; BC 2059;
NCI Metathesaurus CUI : CL562695;
Origin ID : C155885;
UMLS CUI : C4744432;
Semantic type(s)
concept_is_in_subset
has_target