General description

A cell-permeable purine compound that binds ARFGAPs (K_d = 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/β-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 µM).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Zhang, Q., et al. 2007. Proc. Natl. Acad. Sci. USA104, 7444.

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Regulatory Review (Z)