| Description | KY-02327, a metabolically stabilized analog of KY-02061, serves as a potent inhibitor of the Dishevelled (Dvl)-CXXC5 interaction. This compound activates the Wnt/β-catenin pathway, thereby promoting osteoblast differentiation. |
| In vitro | KY-02327（1-10 μM；2天；MC3T3E1细胞，一种小鼠前骨母细胞系）以剂量依赖的方式增加β-catenin蛋白水平，并与Runx2一起促进核内β-catenin的积累[1]。此外，KY-02327（1-10 μM）提高了胶原蛋白1a（Col1a）和骨钙素（OCN），即成骨细胞分化标志物的mRNA水平[1]。 |
| In vivo | KY-02327（20 mg/kg；口服；每周连续五天，为期四周）在去卵巢（OVX）小鼠模型中成功抑制了骨质流失，展现出作为发展骨骼阳性抗骨质疏松药物的潜力[1]。动物模型：8周龄雌性BL6小鼠（经去卵巢（OVX）诱导的骨质疏松模型小鼠）[1]。剂量：20 mg/kg。给药方式：口服；连续给药5天，每周一次，持续四周。结果：与接受载体处理的OVX小鼠相比，其股骨中用calcein标记的新形成骨骼减少。 |
| molecular weight | 373.45 |
| Molecular formula | C20H27N3O4 |
| CAS | 2093407-25-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 100 mg/mL (267.77 mM), Sonication is recommended. |
| References | 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. |