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XAV939
Cayman Chemical Item Number 13596
(CAS 284028-89-3)
XAV939 (CAS 284028-89-3)
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- Inhibitors (475)
- Cancer (556)
- Signal Transduction (302)
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Description
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 β-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 proteins1, tankyrases promote axin ubiquitination, possibly through poly-ADP-ribosylation (PARsylation).2 XAV939 is a potent, small molecule inhibitor of tankyrase (TNKS) 1 and 2 with IC50 values of 11 and 4 nM, respectively.2 By inhibiting TNKS activity, XAV939 increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin in SW480 cells.2 At concentrations as low as 0.33 µM, XAV939 inhibits colony formation of APC-deficient colorectal cancer cells.2
1 Smith, S., Giriat, I., Schmitt, A., et al. Tankyrase, a poly(ADP-ribose) polymerase at human telomeres. Science 282 1484-1487 (1998 Nov).
2 Huang, S.A., Mishina, Y.M., Liu, S., et al. Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling. Nature 461 614-619 (2009).
| 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 |
| Formulation |
A crystalline solid |
| Purity |
≥98% |
| Stability |
2 years |
| Storage |
-20°C |
| Shipping |
Wet ice in continental US; may vary elsewhere |
| SMILES |
OC1=NC(C2=CC=C(C(F)?(F)?F)?C=C2)?=NC3=C1CSCC3 |
Background Reading
Huang, S.A., Mishina, Y.M., Liu, S., et al. Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling. Nature 461 614-619 (2009).
Smith, S., Giriat, I., Schmitt, A., et al. Tankyrase, a poly(ADP-ribose) polymerase at human telomeres. Science 282 1484-1487 (1998 Nov).