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IWR-1-endo is a small molecule inhibitor of Wnt Response with IC50 value of 180nM [1].

IWR-1-endo is a small molecule antagonists of the Wnt/β-catenin pathway screened out from a diverse synthetic chemical library. It acts as an inhibitor of Wnt response. IWR-1-endo can inhibit the activity of Wnt1, 2 and 3. In cultured cells, IWR-1-endo inhibits Wnt-induced β-catenin accumulation which is a downstream event of Lrp6 and Dvl2. It is proved that IWR-1-endo promote β-catenin destruction through promoting stability of Axin-scaffolded destruction complexes in the DLD-1 colorectal cancer (CRC) cell line. IWR-1-endo is also shown to inhibit tailfin regeneration and epithelial stem cell self-renewal in zebrafish. These two processes are both dependent on Wnt/β-catenin signaling. Furthermore, IWR-1-endo can block aberrant cell growth supported by hyperactivation of Wnt/β-catenin resulting from Apc loss [1].

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