KY-02327 acetate 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 acetate 对 Wnt/β-catenin 途径具有激活作用，从而促进成骨细胞分化。
货号:ajcx39422
CAS:N/A
分子式:C22H31N3O6
分子量：433.5
溶解度:DMSO : 50 mg/mL (115.34 mM; ultrasonic and warming and heat to 60°C)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

KY-02327 acetate, a metabolically stabilized KY-02061 analog, is a potent Dishevelled (Dvl)-CXXC5 interaction inhibitor. KY-02327 acetate 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) acetate increases β-catenin protein level together with Runx2 and accumulated nuclear β-catenin in a dose-dependent manner[1].KY-02327 (1-10 μM) acetate 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) acetate 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.