(5Z)-5-[[5-(4-Nitrophenyl)-2-furanyl]methylene]-4-oxo-2-thioxo-3-thiazolidinepropanoic acid potassium salt | (Z)-3-(5-((5-(4-nitrophenyl)furan-2-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)propanoic acid potassium salt, KYA1797 potassium salt
规格或纯度
≥96%
英文名称
KYA 1797K
生化机理
Wnt /β-catenin信号抑制剂(IC50 = 0.75μM)。增加β-catenin对毒素,GSK-3β和β-TrCP的结合亲和力。促进破坏复合物的形成,GSK-3β的活化以及β-catenin和K-Ras的磷酸化,导致它们通过遍在蛋白/蛋白酶体系统降解。在体外和小鼠异种移植模型中降低β-catenin和K-Ras的水平并抑制结直肠癌(CRC)细胞的生长。KYA1797K is an inhibitor of both Wnt/β-catenin and Ras pathways. It binds to the axin regulators of the G-protein signaling (RGS) domain enhancing formation of the β-catenin destruction complex and inducing activation GSK3β, which results in phosphorylation and subsequent degradation of both β-catenin and K-Ras. KYA1797K was show to suppress tumor growth and progression in mouse xenografts of CRC cells that had APC and K-Ras mutations.