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Tankyrase Inhibitor

No.174(July 2017)
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)

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