XAV939 is a potent, small molecule inhibitor of tankyrase (TNKS) 1 and 2 (IC50 = 11 and 4 nM, respectively) (Huang et al.) By inhibiting TNKS activity, XAV939 increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin in SW480 cells (Huang et al.), thereby inhibiting WNT pathway downstream actions
Induces cardiomyogenesis in mesoderm progenitor cells derived from mouse embryonic stem cells (Wang et al.)
In combination with the SMAD inhibitors LDN193189 and SB431542, promotes induction of forebrain fates in human pluripotent stem cell lines (Maroof et al.)
Inhibits colony formation of APC-deficient, β-catenin-dependent DLD-1 colorectal cancer cells (Huang et al.)