|Appearance||White to off-white solid.|
|Solubility||Soluble in DMSO or DMF.|
|Other Product Data||
Note: Sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, dissolve first in DMSO and then dilute with the aqueous buffer of choice. Solubility in a 1:3 solution of DMSO:PBS (pH 7.2) (~0.25 mg/ml). It is recommended to use fresh aqueous solutions and not to store them for more than one day.
|Shipping and Handling|
|Short Term Storage||+4°C|
|Long Term Storage||-20°C|
|Handling Advice||Protect from light.|
|Use/Stability||Stable for at least 2 years after receipt when stored at -20°C.|
|Product Specification Sheet|
- Potent and reversible cell permeable Wnt pathway signaling inhibitor [1, 2, 4, 5].
- Inhibits Wnt-induced accumulation of β-catenin, leading to proteasomal degradation of this protein through a destruction complex which consists of Apc, Axin2, CK1 and GSK-3β. Stabilizes the destruction complex, increasing the level of Axin2 protein without changing the levels of Apc or GSK-3β.
- Tankyrase-1 (TNKS1/PARP5a) and Tankyrase-2 (TNKS2/PARP5b) inhibitor (in vitro auto-PARsylation assay) [3, 6].
- Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer: B. Chen, et al.; Nat. Chem. Biol. 5, 100 (2009)
- Structure-activity relationship studies of small-molecule inhibitors of Wnt response: J. Lu, et al.; Bioorg. Med. Chem. Lett. 19, 3825 (2009)
- Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling: S.M. Huang, et al.; Nature 461, 614 (2009)
- Wnt signaling is required for early development of zebrafish swimbladder: A. Yin, et al.; PLoS One 6, e18431 (2011)
- Perturbation of zebrafish swimbladder development by enhancing Wnt signaling in Wif1 morphants: A. Yin, et al.; Biochim. Biophys. Acta 1823, 236 (2012)
- Structural basis of selective inhibition of human tankyrases: M. Narwal, et al.; J. Med. Chem. 55, 1360 (2012)