KY-02327 是代谢稳定的 KY-02061 类似物，是一种有效的 Dishevelled (Dvl)-CXXC5 相互作用抑制剂。KY-02327 对 Wnt/β-catenin 途径具有激活作用，从而促进成骨细胞分化。
KY-02327, a metabolically stabilized KY-02061 analog, is a potent Dishevelled (Dvl)-CXXC5 interaction inhibitor. KY-02327 shows an activating effect on the Wnt/β-catenin pathway, resulting in promotion of osteoblast differentiation[1].
KY-02327 (1-10 μM; 2 days; MC3T3E1 cells, a murine pre-osteoblast cell line) increases β-catenin protein level together with Runx2 and accumulated nuclear β-catenin in a dose-dependent manner[1].KY-02327 (1-10 μM) increases the mRNA levels of osteoblast differentiation markers collagen 1a (Col1a) and osteocalcin (OCN)[1].
KY-02327 (20 mg/kg; p.o.; 5 sequential days per week for 4 weeks) successfully rescues bone loss in the ovariectomized (OVX) mouse model[1].
[1]. Kim HY, et al. Small molecule inhibitors of the Dishevelled-CXXC5 interaction are new drug candidates for bone anabolic osteoporosis therapy. EMBO Mol Med. 2016;8(4):375-387.
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