FzM1 是卷曲受体 FZD4 的负变构调节剂 (NAM)。 FzM1 降低 WNT5A 依赖性 WNT 反应元件 (WRE) 活性 (log EC50inh=-6.2)。 FzM1 与位于 FZD4 的细胞内环 3 (ICL3) 的变构结合位点结合并改变受体的构象，最终抑制 WNT/β-连环蛋白级联。
| Cas No. | 1680196-54-6 |
| Canonical SMILES | O=C(NC1=CC(O)=CC(C2=CC=CS2)=C1)NC3=CC4=CC=CC=C4C=C3 |
| 分子式 | C21H16N2O2S |
| 分子量 | 360.4 |
| 溶解度 | DMF: 12 mg/ml,DMF:PBS (pH 7.2)(1:3): 0.2 mg/ml,DMSO: 10 mg/ml |
| 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 | Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis. Wnt proteins initiate cell signaling by binding Frizzled (Fz) receptors, a family of G protein-coupled receptors. FzM1 is an allosteric ligand of Fz4. At 10 µM, it inhibits nuclear translocation of β-catenin in U87MG glioma cells treated with lithium chloride, a GSK3 inhibitor that enhances the Wnt canonical signaling pathway. FzM1 impairs the ability of U87MG cells to form neurospheres in culture and stimulates the differentiation of Caco-2 epithelial colorectal adenocarcinoma cells. |
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