044963
CAS Number
1127442-82-3Grade
Highly PurifiedMolecular Formula
C₂₅H₁₉N₃O₃Molecular Weight
409.4EU Commodity Code
38220090Shipping Temp
Blue IceStorage Temp
4°C/-20°CIWR-1 (IWR-1-endo)
4-[(3aR,4S,7R,7aS)-1,3,3a,4,7,7a-Hexahydro-1,3-dioxo-4,7-methano-2H-isoindol-2-yl]-N-8-quinolinylbenzamide
Potent and reversible cell permeable Wnt pathway signaling inhibitor. 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).
Synonyms
rel-4-[(3aR,4S,7R,7aS)-1,3,3a,4,7,7a-hexahydro-1,3-dioxo-4,7-methano-2H-isoindol-2-yl]-N-8-quinolinylbenzamide
Molecular Formula
C₂₅H₁₉N₃O₃
Appearance
White to off-white solid.
Solubility
Soluble in DMSO or DMF. 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) (~0.25mg/ml). It is recommended to use fresh aqueous solutions and not to store them for more than one day.
Storage and Stability
Short-term Storage: +4°C Long-term Storage: -20°C Stable for at least 2 years after receipt when stored at -20°C.
Important Note
This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.
Intended for research use only. Not for use in human, therapeutic, or diagnostic applications.
References
● 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)USBio References
No references available