XAV939

The Wnt signaling pathway is integral to normal biological processes and inappropriately active in many cancers. It is regulated through degradation of the downstream effector beta-catenin via a complex consisting of the tumor suppressor APC, axin, and glycogen synthase kinase 3 (GSK3). Axin is the concentration-limiting factor for this degradation complex. Initially indentified as telomere-associated proteins, tankyrases promote axin ubiquitination, possibly through poly-ADP-ribosylation (PARsylation). XAV939 is a potent, small molecule inhibitor of tankyrase (TNKS) 1 and 2 with IC50 values of 11 and 4 nM, respectively. By inhibiting TNKS activity, XAV939 increases the protein levels of the axin-GSK3beta complex and promotes the degradation of beta-catenin in SW480 cells. At concentrations as low as 0.33 µM, XAV939 inhibits colony formation of APC-deficient colorectal cancer cells.Formal Name: 3,5,7,8-tetrahydro-2-[4-(trifluoromethyl)phenyl]-4H-thiopyrano[4,3-d]pyrimidin-4-one. CAS Number: 284028-89-3. Molecular Formula: C14H11F3N2OS. Formula Weight: 312.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMF:PBS (pH 7.2) (1:5): 0.15 mg/ml, DMSO: 2 mg/ml. SMILES: OC1=NC(C2=CC=C(C(F)(F)F)C=C2)=NC3=C1CSCC3. InChi Code: InChI=1S/C14H11F3N2OS/c15-14(16,17)9-3-1-8(2-4-9)12-18-11-5-6-21-7-10(11)13(20)19-12/h1-4H,5-7H2,(H,18,19,20). InChi Key: KLGQSVMIPOVQAX-UHFFFAOYSA-N. Origin: Synthetic.