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Description

A cell-permeable, biarylurea derivative that acts as a reversible inhibitor of Wnt-b-catenin signaling (EC50 = 5.74 µ,M). 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 µ,M). Also reported to abolish Norrin-dependent TCF/LEF activation and gene transcription in HEK293 cells.