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 b-catenin, leading to proteasomal degradation of this protein through a destruction complex which consists of Apc, Axin2, CK1 and GSK-3b. Stabilizes the destruction complex, increasing the level of Axin2 protein without changing the levels of Apc or GSK-3b. Tankyrase-1 (TNKS1/PARP5a) and Tankyrase-2 (TNKS2/PARP5b) inhibitor (in vitro auto-PARsylation assay).\n\nStorage and Stability:\nShort-term Storage: +4 degrees C\nLong-term Storage: -20 degrees C\nStable for at least 2 years after receipt when stored at -20 degrees C.

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SPECIFICATIONS

Catalog Number

044963

Size

5mg

Purity

>98%

References

Product Reference: ? 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)

Alternative Names

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