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KY-02327 is an orally active, small molecule inhibitor of the Dishevelled (Dvl)-CXXC5 interaction with IC50 of 3.1 uM, a metabolically stabilized KY-02061 analog; KY-02327 is more stable by 2.3-fold and 1.3-fold than KY-02061 in rat liver microsomes and in human hepatocytes, respectively; shows enhanced effect on induction of ALP activity of osteoblast cells compared with KY-02061; activates the Wnt/β-catenin pathway, promotes osteoblast differentiation, and rescues BMD, bone volume, and trabecular bone structures in variectomized (OVX) mouse model.



2093406-88-1 KY-02061 is a small-molecule inhibitor of Dishevelled-CXXC5 interaction with IC50 of 24 uM in vitro binding assay; increases the activation of the Wnt/β-catenin pathway in a dose-dependent manner as revealed by the TOPflash reporter assay, ALP activity also increased in a dose‐dependent manner in KY-02061-treated primary osteoblast cells, increases levels of Runx2, an osteoblast differentiation marker, and β-catenin

NSC 668036

144678-63-7 NSC 668036 is a specific inhibitor of the Dishevelled (Dvl) PDZ domain, extremely weakly binds to PSD-95, PSD95, and PDZ7 domain of GRIP; inhibits the signaling induced by Wnt3A and blocks Wnt signaling by interrupting the Fz-Dvl interaction; suppresses β-catenin-driven gene transcription and abolishes TGF-β1-induced migration, expression of collagen I and α-α-SMA in fibroblasts; depresses fibrotic process in vivo.

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