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Description

A cell-permeable amidobenzanilide compound that disrupts Fz-Dvl (frizzled-dishevelled) interaction by targeting the PDZ domain (Kd = 10.6 µ,M) of Dvl, blocking Wnt3a-induced (10 ng/ml) transcription activity (~50% inhibition at 3 µ,M in 293 cell SuperTopflash reporter assays) and suppressing the Wnt pathway-dependent growth of prostate cancer PC-3 cells (by 16% in 72 h at >=50 µ,M, IC50 = 12.5 µ,M). Shown to effectively prevent Wnt3A mRNA injection-induced xenopus embryo deformation (effective conc. = 25 µ,M) and suppress Wnt pathway-mediated apoptosis of the hyaloid vescular endothelial cells in the mouse eyes via vitreous injection (144 fmol/120 nl/eye) in vivo.