XAV 939

Catalog # Availability Size / Price Qty
3748/10
3748/50
XAV 939 | CAS No. 284028-89-3 | Tankyrase Inhibitors
1 Image
Description: Potent tankyrase inhibitor

Chemical Name: 3,5,7,8-Tetrahydro-2-[4-(trifluoromethyl)phenyl]-4H-thiopyrano[4,3-d]pyrimidin-4-one

Purity: ≥98%

Product Details
Citations (41)
Supplemental Products
Reviews (1)

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. 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
  2. Tankyrase inhibition stabilizes axin and antagonizes wnt signalling.
    Huang et al.
    Nature, 2009;461:614
  3. Inhibiting wnt signaling.
    Adler
    Sci.Signal., 2009;91

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Citations for XAV 939

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

41 Citations: Showing 1 - 10

  1. Human iPS cell-derived engineered heart tissue does not affect ventricular arrhythmias in a guinea pig cryo-injury model.
    Authors: Pecha Et al.
    Sci Rep  2019;9:9831
  2. Distinct Molecular Trajectories Converge to Induce Naive Pluripotency.
    Authors: Stuart Et al.
    Cell Stem Cell  2019;25:388
  3. Reliability of human cortical organoid generati
    Authors: Yoon Et al.
    Nat Methods  2019;16:75
  4. Capacitation of human na�ve pluripotent stem cells for multi-lineage differentiation.
    Authors: Rostovskaya Et al.
    Development  2019;146
  5. Dynamics of genome reorganization during human cardiogenesis reveal an RBM20-dependent splicing factory.
    Authors: Bertero Et al.
    Nat Commun  2019;10:1538
  6. MERIT40-dependent recruitment of tankyrase to damaged DNA and its implication for cell sensitivity to DNA-damaging anticancer drugs.
    Authors: Okamoto Et al.
    Oncotarget  2018;9:35844
  7. Heparanase attenuates axon degeneration following sciatic nerve transection.
    Authors: Whitehead
    Sci Rep  2018;8(1):5219
  8. Polysome profiling followed by RNA-seq of cardiac differentiation stages in hESCs.
    Authors: Pereira Et al.
    Sci Data  2018;5:180287
  9. Quantification of Total and Mutant Huntingtin Protein Levels in Biospecimens Using a Novel alphaLISA Assay.
    Authors: Baldo Et al.
    Eneuro  2018;5
  10. Exit from Naive Pluripotency Induces a Transient X Chromosome Inactivation-like State in Males.
    Authors: Sousa Et al.
    Cell Stem Cell  2018;22:919
  11. β-Catenin Directs Nuclear Factor-κB p65 Output via CREB-Binding Protein/p300 in Human Airway Smooth Muscle.
    Authors: Koopmans Et al.
    Front Immunol  2017;8:1086
  12. Specification of murine ground state pluripotent stem cells to regional neuronal populations.
    Authors: Alsanie
    Sci Rep  2017;7(1):16001
  13. Derivation of telencephalic oligodendrocyte progenitors from human pluripotent stem cells.
    Authors: Major Et al.
    Curr Protoc Stem Cell Biol  2017;39:1H.10.1
  14. Degree of tissue differentiation dictates susceptibility to BRAF-driven colorectal cancer.
    Authors: Tong
    Cell Rep  2017;21(13):3833
  15. Circadian networks in human embryonic stem cell-derived cardiomyocytes.
    Authors: Dierickx Et al.
    EMBO Rep  2017;18:1199
  16. 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
  17. The doublesex-related Dmrta2 safeguards neural progenitor maintenance involving transcriptional regulation of Hes1.
    Authors: Young
    Proc Natl Acad Sci U S A.  2017;114(28):E5599
  18. Selective targeting of CREB-binding protein/β-catenin inhibits growth of and extracellular matrix remodelling by airway smooth muscle.
    Authors: Koopmans Et al.
    Br J Pharmacol  2016;173:3327
  19. Generating high-purity cardiac and endothelial derivatives from patterned mesoderm using humanpluripotent stem cells
    Authors: Palpant Et al.
    Nature Protocols  2016;12:15
  20. Wnt/β-catenin signaling promotes self-renewal and inhibits the primed state transition in na�ve human embryonic stem cells.
    Authors: Xu Et al.
    Proc Natl Acad Sci U S A  2016;113:E6382
  21. 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
  22. β-catenin promotes regulatory T-cell responses in tumors by inducing vitamin A metabolism in dendritic cells.
    Authors: Hong Et al.
    Cancer Res  2015;75:656
  23. Plasticity of Hopx(+) type I alveolar cells to regenerate type II cells in the lung.
    Authors: Jain Et al.
    Nat Commun  2015;6:6727
  24. Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
    Authors: Mallinger Et al.
    J Med Chem  2015;58:1717
  25. A balance of positive and negative regulators determines the pace of the segmentation clock.
    Authors: Wiedermann Et al.
    Elife  2015;4
  26. MRT-92 inhibits Hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor.
    Authors: Hoch Et al.
    FASEB J  2015;29:1817
  27. Neural cells play an inhibitory role in pancreatic differentiation of pluripotent stem cells.
    Authors: Nakashima Et al.
    Genes Cells  2015;20:1028
  28. Prostaglandin E2 promotes MYCN non-amplified neuroblastoma cell survival via β-catenin stabilization.
    Authors: Jansen Et al.
    Blood  2015;19:210
  29. 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
  30. 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
  31. 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
  32. A zebrafish chemical suppressor screening identifies small molecule inhibitors of the Wnt/β-catenin pathway.
    Authors: Nishiya Et al.
    Chem Biol  2014;21:530
  33. Critical roles of p53 in epithelial-mesenchymal transition and metastasis of hepatocellular carcinoma cells.
    Authors: Wang Et al.
    Genome Biol  2013;8:e72846
  34. 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
  35. WNT3 is a biomarker capable of predicting the definitive endoderm differentiation potential of hESCs.
    Authors: Jiang Et al.
    Stem Cell Reports  2013;1:46
  36. Transmembrane protein 88: a Wnt regulatory protein that specifies cardiomyocyte development.
    Authors: Palpant Et al.
    Development  2013;140:3799
  37. BMP-mediated specification of the erythroid lineage suppresses endothelial development in blood island precursors.
    Authors: Myers and Krieg
    Blood  2013;122:3929
  38. WLS inhibits melanoma cell proliferation through the β-catenin signalling pathway and induces spontaneous metastasis.
    Authors: Yang Et al.
    EMBO Mol Med  2012;4:1294
  39. 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
  40. Axin2 as regulatory and therapeutic target in newborn brain injury and remyelination.
    Authors: Fancy Et al.
    Nat Neurosci  2011;14:1009
  41. NKG2D receptor regulates human effector T-cell cytokine production.
    Authors: Barber and Sentman
    Cell Res  2011;117:6571

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Wnt signaling inhibitor
By Kishor Pant on 05/22/2019
Species: Human

XAV 393 inhibits the B-catenin expression in cancer cells in-vitro at 500nM.


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