FzM1 (Synonyms: Frizzled M1) |
| カタログ番号GC41534 |
FzM1 は Frizzled 受容体 FZD4 のネガティブ アロステリック モジュレーター (NAM) です。 FzM1 は、WNT5A 依存性 WNT 応答エレメント (WRE) 活性を低下させます (log EC50inh=-6.2)。 FzM1 は、FZD4 の細胞内ループ 3 (ICL3) にあるアロステリック結合部位に結合し、受容体の立体構造を変化させ、最終的に WNT/β-カテニンカスケードを阻害します。
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Cas No.: 1680196-54-6
Sample solution is provided at 25 µL, 10mM.
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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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