IWR-1 (IWR-1-endo) is a tankyrase inhibitor targeting Wnt/β-catenin ( IC 50 = 180 nM). IWR-1 compromises critical steps of the canonical Wnt signaling , namely translocation of β-catenin to the nucleus and subsequent TCF/LEF activation and expression of Wnt/β-catenin downstream targets. IWR-1 promotes β-catenin phosphorylation by promoting stability of Axin-scaffolded destruction complexes. IWR-1 can be studied in research for anti-tumor purposes, and diseases such as osteosarcoma, colorectal cancer and psoriasis.
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