XAV-939

Tankyrase inhibitor (IC50=11 and 4 nM for TNKS1 and 2 respectively). Antagonizes Wnt signaling downstream of receptor activation via stabilization of axin, a negative regulator of β-catenin [1]. Robustly induces cardiomyogenesis of stem cells [2]. Reduces experimental fibrosis in a mouse model of bleomycin-induced dermal fibrosis [3]. Promotes apoptosis in a neuroblastoma cell line via telomere shortening [4]. An important tool for probing the activation of the Wnt/β-catenin pathway in cells [5]. Cell permeable.

References:

1) S. Huang et al. Nature 2009 46:614

2) H Wang et al. ACS Chem. Biol. 2011 6:192

3) A Distler Wang et al. Ann. Rheum. Dis. 2013 72:1575

4) X Tian et al. Oncol. Rep. 2014 32:1999

5) KC Davidson et al. Proc. Natl. Acad. Sci. USA 2012 109:4485