Tegavivint, ß-Catenin pathway inhibitor (TBI4642)

Description

Product Details

Formal Name: rel-2,7-Bis[[(3R,5S)-3,5-dimethylpiperidin-1-yl]sulfonyl]antracene-9,10-dione dioxime

Alternate Names: BC2059; Tegatrabetan

Molecular Formula: C₂₈H₃₆N₄O₆S₂

Formula Weight: 588.7

CAS Number: 1227637-23-1

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Storage: -20°C

Stability: ≥ 2 years.

Applications

ß-Catenin pathway inhibitor

Functions

Potent inhibitor (IC₅₀ = <10 nM) of the ß-catenin pathway. Active in vitro in multiple cancer cells with nanomolar potency. Displayed efficacy in mouse models of acute myeloid leukemia, multiple myeloma, and mantle cell lymphoma. 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. This interaction does not effect Notch, Sonic Hedgehog, or Hippo signaling pathways. Promotes a lipid-dependent nonapoptotic cell death that is dependent on the enzyme trans-2,3-enoyl-CoA reductase (TECR).

Application Procedures

First dissolved in DMSO (up to at least 25 mg/ml, then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.

Research use only.

Additional information

Datasheet:

TBI4642_Tegavivint_Datasheet

MSDS:

TBI4642_Tegavivint_MSDS

Research use only.