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Formula
C21H16N2O2S
MW
360.43
Purity
>90%
Mode Of Action
inhibitor
Research Area
NEUROLOGY
Bio Chemical Notes
An allosteric ligand of the Frizzled4 (Fz4) receptor and a Wnt/β-catenin pathway inhibitor. FzM1 is believed to induce conformational changes in Fz4 by interacting with the third intracellular loop, ICL3, inhibiting binding of dishevelled (Dsh) and hampering the formation of the Fz4-Dsh complex that is necessary for β-catenin nuclear transport and ultimately transcription of TCF/LEF-regulated genes. FzM1 was tested on two tumor cell lines. U87MG glioblastoma cells acquired a more differentiated phenotype on application. FzM1 and FzM1alk also sped up the differentiation of Caco-2 cells. FzM1 has a log EC50 value of 5.74 for inhibition of Wnt antagonism