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XAV939
WNT pathway inhibitor; Inhibits TNKS1 and TNKS2
XAV939
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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.
DIFFERENTIATION
- 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.).
CANCER RESEARCH
- Inhibits colony formation of APC-deficient, β-catenin-dependent DLD-1 colorectal cancer cells (Huang et al.).
