Wnt-beta-Catenin Signaling Inhibitor, FzM1

Descrição detalhada : A cell-permeable, biarylurea derivative that acts as a reversible inhibitor of Wnt-b-catenin signaling (EC50 = 5.74 µM). Acts by blocking the phosphorylation and nuclear translocation of beta-catenin thereby reduces the transcription of TCF/LEF-regulatory genes. Also shown to block TCF/LEF activation induced by lithium chloride. However, it does not affect GSK3-beta or the APC destruction complex. Induces con-formational changes in Fz4-WT that ultimately allow it to inhibit beta-catenin nuclear transport. Shown to promote HA-Fz4-FEVR plasma membrane localization in U87MG glioblastoma cells and Caco-2 cells (~ 10 µM). Also reported to abolish Norrin-dependent TCF/LEF activation and gene transcription in HEK293 cells.
Sinónimos : Wnt-beta-Catenin Signaling Inhibitor, FzM1; Frizzled4 Modulator, FzM1
Fórmula molecula r: C21H16N2O2S
Armazenamento : -20C
Embalagem : 1X1EA