Tankyrase Inhibitor

No.174(July 2017)

X0077: XAV 939 (1)

XAV 939 (1), which was discovered by a chemical genetic screening, is a small molecule inhibitor of tankyrase.¹⁾ 1 inhibits tankyrase 1 and 2 with IC₅₀ values of 11 and 4 nM, respectively (Table). Inhibition of tankyrase by 1 stabilizes axin, resulting in stimulating β-catenin degradation. The destabilization of β-catenin inhibits Wnt signal pathway. Therefore, 1 is used as an antagonist of Wnt signaling.

β-Catenin plays important roles in pluripotency of stem cells.²⁾ Davidson et al. reported that loss of hESCs self-renewal is promoted by activation of Wnt/β-catenin signaling and 1 blocks the loss.³⁾ In addition, conversion of mouse EpiSCs to naïve-like PSCs (rESCs)　is enhanced by inhibition of nuclear translocation of β-catenin with 1.⁴⁾ 1 also induces cardiomyocyte differentiation from mouse and human ESCs.^5,6)

EpiSCs: epiblast stem cells
PSCs: pluripotent stem cells
rESCs: reverted embryonic stem cells

Table. Inhibitoryactivity of XAV 939¹⁾

The product is for research purpose only.

References

1)Tankyrase inhibition stabilizes axin and antagonizes Wnt signaling
- S.-M. A. Huang, Y. M. Mishina, S. Liu, A. Cheung, F. Stegmeier, G. A. Michaud, O. Charlat, E. Wiellette, Y. Zhang, S. Wiessner, M. Hild, X. Shi, C. J. Wilson, C. Mickanin, V. Myer, A. Fazal, R. Tomlinson, F. Serluca, W. Shao, H. Cheng, M. Shultz, C. Rau, M. Schirle, J. Schlegl, S. Ghidelli, S. Fawell, C. Lu, D. Curtis, M. W. Kirschner, C. Lengauer, P. M. Finan, J. A. Tallarico, T. Bouwmeester, J. A. Porter, A. Bauer, F. Cong, Nature 2009, 461, 614.
2)β-Catenin in pluripotency: Adhering to self-renewal or wnting to differentiate?
- G. S. Sineva, V. A. Pospelov, Int. Rev. Cell Mol. Biol. 2014, 312, 53.
3)β-catenin signaling promotes differentiation, not self-renewal, of human embryonic stem cells and is repressed by Oct4
- K. C. Davidson, A. M. Adams, J. M. Goodson, C. E. McDonald, J. C. Potter, J. D. Berndt, T. L. Biechele, R. J. Taylor, R. T. Moon, Proc. Natl. Acad. Sci. USA 2012, 109, 4485.
4)Successful reprogramming of epiblast stem cells by blocking nuclear localization of β-catenin
- H. Murayama, H. Masaki, H. Sato, T. Hayama, T. Yamaguchi, H. Nakauchi, Stem Cell Rep. 2015, 4, 103.
5)Cardiac induction of embryonic stem cells by a small molecule inhibitor of Wnt/β-catenin signaling
- H. Wang, J. Hao, C. C. Hong, ACS Chem. Biol. 2011, 6, 192.
6)Small-molecule inhibitors of the Wnt pathway potently promote cardiomyocytes from human embryonic stem cell-derived mesoderm
- E. Willems, S. Spiering, H. Davidovics, M. Lanier, Z. Xia, M. Dawson, J. Cashman, M. Mercola, Circ. Res. 2011, 109, 360.

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Tankyrase Inhibitor

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