Catalog Number: 3748
Chemical Name: 3,5,7,8-Tetrahydro-2-[4-(trifluoromethyl)phenyl]-4H-thiopyrano[4,3-d]pyrimidin-4-one
Biological Activity
Potent tankyrase (TNKS) inhibitor (IC50 values are 4 and 11 nM for TNKS2 and TNKS1 respectively). Antagonizes Wnt signaling via stimulation of β-catenin degradation and stabilization of axin. Inhibits proliferation of the β-catenin-dependent colon carcinoma cell line DLD-1. Promotes cardiomyogenic development in mesoderm progenitor cells.
External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of XAV939 is reviewed on the chemical probes website.
Technical Data
  • M.Wt:
    312.31
  • Formula:
    C14H11F3N2OS
  • Solubility:
    Soluble to 20 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at RT
  • CAS No:
    284028-89-3
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Tankyrase inhibition stabilizes axin and antagonizes wnt signalling.
    Huang et al.
    Nature, 2009;461:614
  2. Cardiac induction of embryonic stem cells by a small molecule inhibitor of Wnt/β-catenin signaling.
    Wang et al.
    ACS Chem. Biol., 2010;6:192
  3. Inhibiting wnt signaling.
    Adler
    Sci.Signal., 2009;91
Citations:

The citations listed below are publications that use Tocris products. Selected citations for XAV 939 include:

17 Citations: Showing 1 - 10
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  1. Aryl hydrocarbon receptor/cytochrome P450 1A1 pathway mediates breast cancer stem cells expansion through PTEN inhibition and β-Catenin and Akt activation.
    Authors: Al-Dhfyan
    Mol Cancer 2017;16:14
  2. Generating high-purity cardiac and endothelial derivatives from patterned mesoderm using humanpluripotent stem cells
    Authors: Palpant Et al.
    Nature Protocols 2016;12:15
  3. Downregulation of Wnt signaling by sonic hedgehog activation promotes repopulation of human tumor cell lines.
    Authors: Ma Et al.
    J Cell Mol Med 2015;8:385
  4. Plasticity of Hopx(+) type I alveolar cells to regenerate type II cells in the lung.
    Authors: Jain Et al.
    Nat Commun 2015;6:6727
  5. A balance of positive and negative regulators determines the pace of the segmentation clock.
    Authors: Wiedermann Et al.
    Elife 2015;4
  6. Prostaglandin E2 promotes MYCN non-amplified neuroblastoma cell survival via β-catenin stabilization.
    Authors: Jansen Et al.
    Blood 2015;19:210
  7. Statistically based splicing detection reveals neural enrichment and tissue-specific induction of circular RNA during human fetal development.
    Authors: Szabo Et al.
    Dis Model Mech 2015;16:126
  8. Enhanced Electrical Integration of Engineered Human Myocardium via Intramyocardial versus Epicardial Delivery in Infarcted Rat Hearts.
    Authors: Gerbin Et al.
    PLoS One 2015;10:e0131446
  9. Cardiac development in zebrafish and human embryonic stem cells is inhibited by exposure to tobacco cigarettes and e-cigarettes.
    Authors: Palpant Et al.
    PLoS One 2015;10:e0126259
  10. Critical roles of p53 in epithelial-mesenchymal transition and metastasis of hepatocellular carcinoma cells.
    Authors: Wang Et al.
    Genome Biol 2013;8:e72846
  11. Histone H3K27me3 demethylases KDM6A and KDM6B modulate definitive endoderm differentiation from human ESCs by regulating WNT signaling pathway.
    Authors: Jiang Et al.
    ASN Neuro 2013;23:122
  12. WNT3 is a biomarker capable of predicting the definitive endoderm differentiation potential of hESCs.
    Authors: Jiang Et al.
    Stem Cell Reports 2013;1:46
  13. Transmembrane protein 88: a Wnt regulatory protein that specifies cardiomyocyte development.
    Authors: Palpant Et al.
    Development 2013;140:3799
  14. BMP-mediated specification of the erythroid lineage suppresses endothelial development in blood island precursors.
    Authors: Myers and Krieg
    Blood 2013;122:3929
  15. Differential modulation of the oligodendrocyte transcriptome by sonic hedgehog and bone morphogenetic protein 4 via opposing effects on histone acetylation.
    Authors: Wu Et al.
    J Neurosci 2012;32:6651
  16. Axin2 as regulatory and therapeutic target in newborn brain injury and remyelination.
    Authors: Fancy Et al.
    Nat Neurosci 2011;14:1009
  17. NKG2D receptor regulates human effector T-cell cytokine production.
    Authors: Barber and Sentman
    Cell Res 2011;117:6571
Expand to show all 17 Citations

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