Chemical Name: rel-2,7-Bis[[(3R,5S)-3,5-dimethylpiperidin-1-yl]sulfonyl]antracene-9,10-dione dioxime. Alternate Names: BC2059, Tegatrabetan
ß-Catenin pathway inhibitor
Molecular Weight:
588.74
Purity:
98% by HPLC NMR (Conforms)
Form:
Off-white solid
CAS Number:
[1227637-23-1]
Formula:
C28H36N4O6S2
Application Notes:
Tegavivint is a potent inhibitor (IC50 = <10 nM) of the ß-catenin pathway.1 Active in vitro in multiple cancer cells with nanomolar potency. Tegavivint displayed efficacy in mouse models of acute myeloid leukemia2, multiple myeloma3, and mantle cell lymphoma4. It inhibits the ß-catenin pathway in a unique way by selectively binding to Transducin Beta-like related protein 1 (TBLR1) leading to displacement of ß-catenin from the TBL1/ß-catenin complex.5 This interaction does not effect Notch, Sonic Hedgehog, or Hippo signaling pathways. Tegavivint promotes a lipid-dependent nonapoptotic cell death that is dependent on the enzyme trans-2,3-enoyl-CoA reductase (TECR).6
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