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Beschreibung

A cell-permeable purine compound that binds ARFGAPs (Kd = 364 and 620 nM for AMAP1 and ARFGAP1, respectively) and acts as a broad specificity ARFGAPs inhibitor (GTPase activating proteins of ADP-ribosylation factor). Shown to synergize with Wnt-3a and specifically activate the canonical Wnt/beta-catenin signaling pathway both in vitro (2-, 40-, and 200-fold increase of basal transcription activity by QS11, Wnt-3a, and QS11/Wnt-3a, respectively, in a Super(8X)TOPFlash reporter assay using HEK293 cells) and in vivo (in the induction of Xenopus embryonic axis duplication). Also reported to block the migration of AMAP1-overexpressing MDA-MB-231 cells (86% inhibition at 2.5 µ,M).