Cayman Iwr-1-Endo; Purity- Greater Than Or Equal To 98%; Size- 50

Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.^1,2,3 Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWR-1-endo is a potent inhibitor of the Wnt response, blocking a cell-based Wnt/β-catenin pathway reporter response with an IC₅₀ value of 180 nM.⁴ It inhibits, at 10 μM, Wnt-induced accumulation of β-catenin, leading to proteasomal degradation of this protein through a destruction complex which consists of Apc, Axin2, Ck1, and GSK3β. IWR-1-endo stabilizes the destruction complex, increasing the level of Axin2 protein without changing the levels of Apc or GSK3β.⁴ The IWR compound does not change the de novo synthesis of Axin2, alter the affinity of Axin2 for β-catenin, or inhibit the proteasome. It has a half-life of 60 minutes in murine whole blood and 20 minutes in intact murine hepatocytes.⁵ In in vivo tests, IWR-1-endo inhibits zebrafish tail fin regeneration with a minimum inhibitory concentration of 0.5 μM.⁵ The IWR-1-exo diastereomer exhibits much less activity against the Wnt/β-catenin pathway and has been used as a control.⁴

WARNING This product is not for human or veterinary use.