XAV939 is a potent and selective Wnt pathway antagonist. It
functions to stabilize Axin by inhibiting the poly-ADP-ribosylating
enzymes tankyrase 1 and tankyrase 2 with IC50 of 11 nM and 4
nM, respectively. It has been used to study Wnt-dependent cancers. In
addition, XAV939 was shown to stabilize Axin2 level in oligodendrocyte
precursor cells in the spinal cord and accelerated their differentiation
and myelination after hypoxic and demyelinating injury. It can also
robustly induce cardiomyocyte differentiation from mouse and human
ESCs/iPSCs.
How to Use:
- In vitro: XAV939 was used at 1 µM concentration to
stabilize Axin and in stem cell culture. It can be used to functionally
replace Dkk protein in blocking Wnt signaling in many assay conditions
(e.g., 40 times more effective in inducing cardiogenesis than
recombinant Wnt inhibitor protein Dkk).
- 1. Huang SMA, et al. Tankyrase inhibition stabilizes axin and antagonizes Wnt signaling; (2009) Nature. 461, 614-620
Reference:
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2. Wang H, et al. Cardiac induction of embryonic stem cells by a
small molecule inhibitor of Wnt/β-catenin signaling. (2011) ACS Chem
Biol. 6(2):192-7.
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3. Fancy SP, et al. Axin2 as regulatory and therapeutic target in
newborn brain injury and remyelination. (2011) Nat Neurosci.
14(8):1009-16.
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4. Willems E, et al. Small-molecule inhibitors of the Wnt pathway
potently promote cardiomyocytes from human embryonic stem cell-derived
mesoderm. (2011) Circ Res.109(4):360-4.
Products are for research use only. Not for human use.
