|Reconstitution||Before reconstitution, we recommend a brief spin to drive down any material dislodged from the bottom of the tube. The compound is soluble in DMSO.|
|Stability||The powder is stable for at least 2 year if stored at -20 °C. The dissolved compound is stable for at least 1 month at 4 °C, but should be stored in aliquots at -20 °C for longer term. Protect from light.|
|Purity||Greater than 98% as determined by LC/MS analysis. LC/MS and/or NMR data available upon request.|
|Biological Activity||In a cell-based assay measuring the activation of the TCF reporter gene, this compound gives IC50 of 300 nM.|
|Country of Origin|
XAV-939, 2-(4-(trifluoromethyl)phenyl)-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidin-4-one, is an inhibitor of Tankryases with IC50 of 11 and 4nM for Tankyrase 1 and Tankyrase 2, respectively. It stimulates β-catenin degradation by stabilizing axin, resulting in the inhibition of the canonical WNT pathway. Both tankyrase isoforms interact with a highly conserved domain of axin and stimulate its degradation through the ubiquitin-proteasome pathway. Tankryase inhibitors are potential therapeutics for cancers as deregulated Wnt/β-catenin pathway activity has been implicated in many cancers.
Ref: Huang SM et al. Nature. 2009 Oct 1; 461(7264):614-20.