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FzM1 是卷曲蛋白受体 FZD4 的负变构调节剂 (NAM)。 FzM1减少 WNT5A 依赖的 WNT 反应元件 (WRE) 活性 (log EC50inh=-6.2)。 FzM1 与位于 FZD4 细胞内环 3 (ICL3) 的变构结合位点结合并改变受体的构象,从而抑制 WNT/β-连环蛋白级联反应。
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FzM1 是卷曲蛋白受体 FZD4 的负变构调节剂 (NAM)。 FzM1减少 WNT5A 依赖的 WNT 反应元件 (WRE) 活性 (log EC50inh=-6.2)。 FzM1 与位于 FZD4 细胞内环 3 (ICL3) 的变构结合位点结合并改变受体的构象,从而抑制 WNT/β-连环蛋白级联反应。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 496 | 现货 | |
5 mg | ¥ 679 | 现货 | |
10 mg | ¥ 1,160 | 现货 | |
25 mg | ¥ 2,180 | 现货 | |
50 mg | ¥ 3,530 | 现货 | |
100 mg | ¥ 5,450 | 现货 | |
500 mg | ¥ 11,300 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 589 | 现货 |
产品描述 | FzM1, a negative allosteric modulator (NAM) of the Frizzled receptor FZD4, diminishes WNT5A-dependent WNT responsive element (WRE) activity (log EC50inh=−6.2) by binding to an allosteric site on intracellular loop 3 (ICL3) of FZD4. This interaction changes the receptor's conformation and inhibits the WNT/β-catenin signaling pathway. |
体外活性 | FzM1 inhibited Gli activity less efficiently than TCF/LEF activity (log EC50 of −4.6 and −5.7, respectively). On the contrary, it did not modulate CRE activity (log EC50 > −4.0), indicating that it does not influence GPCRs linked to G proteins[2]. |
别名 | FzM-1, FzM 1 |
分子量 | 360.43 |
分子式 | C21H16N2O2S |
CAS No. | 1680196-54-6 |
Smiles | Oc1cc(NC(=O)Nc2ccc3ccccc3c2)cc(c1)-c1cccs1 |
密度 | 1.401 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 65 mg/mL (180.34 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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