FzM1.8 源自 FzM1,是 FZD4 的变构激动剂,pEC50 为 6.4。 FzM1.8 通过在没有任何 WNT 配体的情况下促进 TCF/LEF 转录活性,与 FZD4 结合并激活 WNT/β-连环蛋白途径。 FzM1.8 结合稳定 FZD4,增加对异源三聚体 G 蛋白的亲和力,并刺激 Gβγ 亚基的释放,进而激活 PI3K。
Cas No. | 2204290-85-5 |
Canonical SMILES | OC(=O)C1=CC(O)=CC(NC(=O)NC2=CC3=C(C=CC=C3)C=C2)=C1 |
分子式 | C18H14N2O4 |
分子量 | 322.32 |
溶解度 | Soluble in DMSO |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | Frizzled 4 allosteric agonist (pEC50 = 6.4). Potentiates the β-catenin pathway in the absence of any WNT ligand, by biasing FZD4 signaling toward the FZD4/PI3K axis. Preserves stemness and promotes proliferation of undifferentiated cells. Riccio et al (2018) A negative allosteric modulator of WNT receptor frizzled 4 switches into an allosteric agonist. Biochemistry 57 839 PMID:29293331 |