Novel small molecule activators of β-catenin-mediated signaling pathway: structure-activity relationships of indirubins

Abstract

Based on the β-catenin-drived Wnt activator of bromoindirubin-3′-oxime (BIO), indirubin analogs were evaluated for β-catenin-mediated gene expression. A novel indirubin analog, indirubin-5-nitro-3′-oxime (INO), was considered a potential activator, and structure-activity studies were conducted with indirubins. These data suggest that INO might be a novel Wnt activator and has a potential of signaling regulator in β-catenin-mediated signaling pathways. © 2009 Elsevier Ltd. All rights reserved.