FzM1 (Synonyms: Frizzled M1) |
| Catalog No.GC41534 |
FzM1 est un modulateur allostérique négatif (NAM) du récepteur Frizzled FZD4. FzM1 réduit l'activité de l'élément réactif WNT (WRE) dépendant de WNT5A (log EC50inh = -6,2). FzM1 se lie À un site de liaison allostérique situé dans la boucle intracellulaire 3 (ICL3) de FZD4 et modifie la conformation du récepteur, inhibant finalement la cascade WNT/β-caténine.
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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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