$ 59.00

Select Size:

  • XAV-002, 2 mg59.00
  • XAV-010, 10 mg159.00
  • XAV-050, 50 mg459.00
Add to Cart
Source M.W.312.31 CAS No.284028-89-3
Structural InfoXAV-939
ReconstitutionBefore reconstitution, we recommend a brief spin to drive down any material dislodged from the bottom of the tube.  The compound is soluble in DMSO.
StabilityThe 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.
PurityGreater than 98% as determined by LC/MS analysis. LC/MS and/or NMR data available upon request.
Biological ActivityIn 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.