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，最终抑制 WNT/β-连环蛋白级联反应。

FzM1 is a negative allosteric modulator (NAM) of Frizzled receptor FZD4. FzM1 reduces WNT5A-dependent WNT responsive element (WRE) activity (log EC50inh=–6.2). FzM1 binds to an allosteric binding site located in intracellular loop 3 (ICL3) of FZD4 and alters the conformation of the receptor, ultimately inhibiting the WNT/β-catenin cascade

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].

1680196-54-6

C21H16N2O2S

360.43

FzM-1;FzM 1

DMSO:58.5mg/mL (162.3mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years