
| Biological Activity | |||||||||||||||||||||||||
| Synonyms | Tankyrase inhibitor, XAV 939, XAV-939, NVP-XAV939 | ||||||||||||||||||||||||
| Chemical Name | 2-[4-(trifluoromethyl)phenyl]-1,5,7,8-tetrahydrothiopyrano[4,3-d]pyrimidin-4-one | ||||||||||||||||||||||||
| Application | XAV939 is a potent inhibitor of beta-catenin, TNKS1, and TNKS2 | ||||||||||||||||||||||||
| CAS Number | 284028-89-3 | ||||||||||||||||||||||||
| Purity | ≥98.5% | ||||||||||||||||||||||||
| Molecular Weight | 312.31 | ||||||||||||||||||||||||
| Molecular Formula | C₁₄H₁₁F₃N₂OS | ||||||||||||||||||||||||
| SMILES | OC1=NC(C2=CC=C(C(F)(F)F)C=C2)=NC3=C1CSCC3 | ||||||||||||||||||||||||
| Target & IC50 | Tankyrase 1: IC50 = 11 nM Tankyrase 2: IC50 = 4 nM Protein Wnt-3a: IC50 = 51 nM Catenin beta-1: IC50 = 51 nM (human) |
||||||||||||||||||||||||
| Shipping | Gel Pack | ||||||||||||||||||||||||
| Storage | Store at -20°C | ||||||||||||||||||||||||
|
|||||||||||||||||||||||||
| Solubility | |
| DMSO: 12 mg/mL (38.42 mM) |
| Product Description | |
XAV939 is a potent, small molecule inhibitor of tankyrase 1 (TNKS) (IC50 = 11 nM) and tankyrase 2 (IC50 = 4 nM). By inhibiting TNKS activity, XAV939 increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin in SW480 cells. At concentrations as low as 0.3 μM, XAV939 inhibits colony formation of APC-deficient colorectal cancer cells. |