IWR-1 endo

Wnt signaling proteins are small secreted proteins active in embryonic development, tumorigenesis and tissue homeostasis.  IWR-1 endo is a potent inhibitor of the Wnt response, blocking a cell-based Wnt/β-catenin pathway reporter response with an IC50 of 180nM.  IWR-1 endo 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 Gsk3β. IWR-1-endo stabilizes the destruction complex, increasing the level of Axin2 protein without changing the levels of Apc or Gsk3β. In in vivo tests , IWR-1 endo has been shown to inhibit zebrafish tail fin regeneration at a minimum inhibitory concentration of 0.5 µM.