Home / Tankyrase Inhibitors / XAV 939

XAV 939

Catalog #: 3748
86 Citations Datasheet / COA / SDS
GMP Version Available: TB3748-GMP
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3748/50
XAV 939 | CAS No. 284028-89-3 | Tankyrase Inhibitors
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Description: Potent tankyrase inhibitor
Alternative Names: XAV939 Wnt Signaling 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 (86)
Supplemental Products
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

XAV 939 is a 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. XAV 939 inhibits proliferation of the β-catenin-dependent colon carcinoma cell line DLD-1. Promotes cardiomyocyte differentiation in mesoderm progenitor cells. Also used in neuronal differentiation protocols.

XAV 939 synthesized to cGMP guidelines also available.

For more information about how XAV 939 may be used, see our protocol: Accelerated Induction of Cortical Neurons from hiPSCs

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. Neuroprotective and regenerative roles of intranasal Wnt-3a Administration after focal ischemic stroke in mice
    ZZ Wei, JY Zhang, TM Taylor, X Gu, Y Zhao, L Wei
    J. Cereb. Blood Flow Metab., 2017;0(0):271678X177026.
  2. A new hERG allosteric modulator rescues genetic and drug-induced long-QT syndrome phenotypes in cardiomyocytes from isogenic pairs of patient induced pluripotent stem cells

    EMBO Mol Med, 2016;0(0):.
  3. Isogenic Pairs of hiPSC-CMs with Hypertrophic Cardiomyopathy/LVNC-Associated ACTC1 E99K Mutation Unveil Differential Functional Deficits
    JGW Smith, T Owen, JR Bhagwan, D Mosqueira, E Scott, I Mannhardt, A Patel, R Barriales-, L Monserrat, A Hansen, T Eschenhage, SE Harding, S Marston, C Denning
    Stem Cell Reports, 2018;0(0):.
  4. Oligodendrocyte-encoded HIF function couples postnatal myelination and white matter angiogenesis.
    Yuen T, Silbereis J, Griveau A, Chang S, Daneman R, Fancy S, Zahed H, Maltepe E, Rowitch D
    Cell, 2014;158(2):383-96.
  5. Epigenetic downregulation of SFRP4 contributes to epidermal hyperplasia in psoriasis.
    Bai J, Liu Z, Xu Z, Ke F, Zhang L, Zhu H, Lou F, Wang H, Fei Y, Shi Y, Wang H
    J Immunol, 2015;194(9):4185-98.
  6. Spatiotemporal oscillations of Notch1, Dll1 and NICD are coordinated across the mouse PSM.
    Bone R, Bailey C, Wiedermann G, Ferjentsik Z, Appleton P, Murray P, Maroto M, Dale J
    Development, 2014;141(24):4806-16.
  7. Serum supplemented culture medium masks hypertrophic phenotypes in human pluripotent stem cell derived cardiomyocytes.
    Dambrot C, Braam S, Tertoolen L, Birket M, Atsma D, Mummery C
    J Cell Mol Med, 2014;18(8):1509-18.
  8. Prostaglandin E2 promotes MYCN non-amplified neuroblastoma cell survival via beta-catenin stabilization.
    Jansen S, Holman R, Hedemann I, Frankes E, Elzinga C, Timens W, Gosens R, de Bont E, Schmidt M
    J Cell Mol Med, 2015;19(1):210-26.
  9. Tankyrase inhibition stabilizes axin and antagonizes wnt signalling.
    Huang et al.
    Nature, 2009;461:614
  10. Inhibiting wnt signaling.
    Adler
    Sci.Signal., 2009;91
  11. Chronic aerobic exercise improves insulin sensitivity and modulates Nrf2 and NF?kappaB/IkappaBalpha pathways in the skeletal muscle of rats fed with a high fat diet
    Q Yu, Z Xia, EC Liong, GL Tipoe
    Mol Med Rep, 2019;20(6):4963-4972.
  12. 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

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Citations for XAV 939

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

86 Citations: Showing 1 - 10

  1. Nicotinamide Mononucleotide Prevents Cisplatin-Induced Mitochondrial Defects in Cortical Neurons Derived from Human Induced Pluripotent Stem Cells.
    Authors: Mi-Hyeon Et al.
    Brain Plast  2023;8:143-152
  2. Differentiation of human induced pluripotent stem cells into cortical neural stem cells.
    Authors: Minal Et al.
    Front Cell Dev Biol  2023;10:1023340
  3. Lipid droplet-associated lncRNA LIPTER preserves cardiac lipid metabolism.
    Authors: Shiyong Et al.
    Nat Cell Biol  2023;
  4. Large-scale genome editing based on high-capacity adenovectors and CRISPR-Cas9 nucleases rescues full-length dystrophin synthesis in DMD muscle cells.
    Authors: Karoly Et al.
    Nucleic Acids Res  2022;50:7761-7782
  5. STRAIGHT-IN enables high-throughput targeting of large DNA payloads in human pluripotent stem cells.
    Authors: Yavuz Et al.
    Cell Rep Methods  2022;2:100300
  6. Amniogenesis occurs in two independent waves in primates.
    Authors: Wolf Et al.
    Cell Stem Cell  2022;29:744-759.e6
  7. 8C-like cells capture the human zygotic genome activation program in vitro.
    Authors: Wolf Et al.
    Cell Stem Cell  2022;29:449-459.e6
  8. Dissecting the molecular basis of human interneuron migration in forebrain assembloids from Timothy syndrome.
    Authors: Daniel H Et al.
    Cell Stem Cell  2022;29:248-264.e7
  9. A dual SHOX2:GFP; MYH6:mCherry knockin hESC reporter line for derivation of human SAN-like cells.
    Authors: Xiaolu Et al.
    iScience  2022;25:104153
  10. Ivermectin represses Wnt/β-catenin signaling by binding to TELO2, a regulator of phosphatidylinositol 3-kinase-related kinases.
    Authors: Naoyuki Et al.
    iScience  2022;25:103912
  11. Cell type determination for cardiac differentiation occurs soon after seeding of human-induced pluripotent stem cells.
    Authors: Arjun Et al.
    Genome Biol  2022;23:90
  12. Autophagy modulates cell fate decisions during lineage commitment.
    Authors: Elisabeth Et al.
    Autophagy  2022;18:1915-1931
  13. Use of standard U-bottom and V-bottom well plates to generate neuroepithelial embryoid bodies.
    Authors: Kerensa Et al.
    PLoS One  2022;17:e0262062
  14. Alzheimer risk gene product Pyk2 suppresses tau phosphorylation and phenotypic effects of tauopathy.
    Authors: Suho Et al.
    Mol Neurodegener  2022;17:32
  15. Engineering brain assembloids to interrogate human neural circuits.
    Authors: Omer Et al.
    Nat Protoc  2022;17:15-35
  16. Norepinephrine transporter defects lead to sympathetic hyperactivity in Familial Dysautonomia models.
    Authors: Gerald W Et al.
    Nat Commun  2022;13:7032
  17. A stem cell roadmap of ribosome heterogeneity reveals a function for RPL10A in mesoderm production.
    Authors: Zhen Et al.
    Nat Commun  2022;13:5491
  18. Naïve-like pluripotency to pave the way for saving the northern white rhinoceros from extinction.
    Authors: Dmitry Et al.
    Sci Rep  2022;12:3100
  19. Paraxial mesoderm organoids model development of human somites.
    Authors: Olivier Et al.
    Elife  2022;11
  20. Efficient Gene Expression in Human Stem Cell Derived-Cortical Organoids Using Adeno Associated Virus.
    Authors: Lars M Et al.
    Cells  2022;11
  21. A single cell transcriptional roadmap of human pacemaker cell differentiation.
    Authors: Jiuru Et al.
    Elife  2022;11
  22. The human amniotic epithelium confers a bias to differentiate toward the neuroectoderm lineage in human embryonic stem cells.
    Authors: Wendy Et al.
    Elife  2022;11
  23. Mapping the temporal and spatial dynamics of the human endometrium in vivo and in vitro.
    Authors: Cecilia Et al.
    Nat Genet  2021;53:1698-1711
  24. Resolving cell state in iPSC-derived human neural samples with multiplexed fluorescence imaging.
    Authors: Beth A Et al.
    Commun Biol  2021;4:786
  25. Pathogenic LMNA variants disrupt cardiac lamina-chromatin interactions and de-repress alternative fate genes.
    Authors: Joseph C Et al.
    Cell Stem Cell  2021;28:938-954.e9
  26. Commitment and oncogene-induced plasticity of human stem cell-derived pancreatic acinar and ductal organoids.
    Authors: Ling Et al.
    Cell Stem Cell  2021;28:1090-1104.e6
  27. ELAVL4, splicing, and glutamatergic dysfunction precede neuron loss in MAPT mutation cerebral organoids.
    Authors: Alison M Et al.
    Cell  2021;184:4547-4563.e17
  28. Generation, functional analysis and applications of isogenic three-dimensional self-aggregating cardiac microtissues from human pluripotent stem cells.
    Authors: Viviana Et al.
    Nat Protoc  2021;16:2213-2256
  29. Urokinase-type plasminogen activator-mediated crosstalk between N-cadherin and β-catenin promotes wound healing.
    Authors: Yang Et al.
    J Cell Sci  2021;134
  30. Responsiveness to perturbations is a hallmark of transcription factors that maintain cell identity in vitro.
    Authors: Arun Et al.
    Cell Syst  2021;12:885-899.e8
  31. A comprehensive analysis of gene expression changes in a high replicate and open-source dataset of differentiating hiPSC-derived cardiomyocytes.
    Authors: Sean P Et al.
    Sci Rep  2021;11:15845
  32. A Human 3D Cardiomyocyte Risk Model to Study the Cardiotoxic Influence of X-rays and Other Noxae in Adults.
    Authors: Insa S Et al.
    Cells  2021;10
  33. Urokinase-type plasminogen activator-mediated crosstalk between N-cadherin and β-Catenin promotes wound healing.
    Authors: Yang Et al.
    J Cell Sci  2021;
  34. Cell Type-Specific In Vitro Gene Expression Profiling of Stem Cell-Derived Neural Models.
    Authors: Nadine Et al.
    Cells  2020;9
  35. Variable expression and silencing of CRISPR-Cas9 targeted transgenes identifies the AAVS1 locus as not an entirely safe harbour.
    Authors: Chris Et al.
    F1000Res  2020;8:1911
  36. Intraflagellar Transport Complex B Proteins Regulate the Hippo Effector Yap1 during Cardiogenesis.
    Authors: Benedicte Et al.
    Cell Rep  2020;32:107932
  37. Tissue-Specific Regulation of the Wnt/β-Catenin Pathway by PAGE4 Inhibition of Tankyrase.
    Authors: Geoffrey Et al.
    Cell Rep  2020;32:107922
  38. Norrin restores blood-retinal barrier properties after vascular endothelial growth factor-induced permeability.
    Authors: Cheng-mao Et al.
    J Biol Chem  2020;295:4647-4660
  39. Human-iPSC-Derived Cardiac Stromal Cells Enhance Maturation in 3D Cardiac Microtissues and Reveal Non-cardiomyocyte Contributions to Heart Disease.
    Authors: Abraham J Et al.
    Cell Stem Cell  2020;26:862-879.e11
  40. GAS2 Promotes Cell Proliferation and Invasion and Suppresses Apoptosis in Pediatric T-Cell Acute Lymphoblastic Leukemia and Activates Wnt/β-Catenin Pathway.
    Authors: Yang Et al.
    Onco Targets Ther  2020;13:1099-1108
  41. 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
  42. Generation of ERK-Independent Human and Non-Human Primate Pluripotent Stem Cells.
    Authors: Alejandro Et al.
    Curr Protoc Stem Cell Biol  2019;49:e85
  43. Specification of positional identity in forebrain organoids.
    Authors: Ryan M Et al.
    Nat Biotechnol  2019;37:436-444
  44. Distinct Molecular Trajectories Converge to Induce Naive Pluripotency.
    Authors: Stuart Et al.
    Cell Stem Cell  2019;25:388
  45. Human SNORA31 variations impair cortical neuron-intrinsic immunity to HSV-1 and underlie herpes simplex encephalitis.
    Authors: Marc Et al.
    Nat Med  2019;25:1873-1884
  46. Generation of Blastocyst-like Structures from Mouse Embryonic and Adult Cell Cultures.
    Authors: Juan Carlos Et al.
    Cell  2019;179:687-702.e18
  47. Reliability of human cortical organoid generati
    Authors: Yoon Et al.
    Nat Methods  2019;16:75
  48. Capacitation of human na�ve pluripotent stem cells for multi-lineage differentiation.
    Authors: Rostovskaya Et al.
    Development  2019;146
  49. Dynamics of genome reorganization during human cardiogenesis reveal an RBM20-dependent splicing factory.
    Authors: Bertero Et al.
    Nat Commun  2019;10:1538
  50. 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
  51. Heparanase attenuates axon degeneration following sciatic nerve transection.
    Authors: Whitehead
    Sci Rep  2018;8(1):5219
  52. Polysome profiling followed by RNA-seq of cardiac differentiation stages in hESCs.
    Authors: Pereira Et al.
    Sci Data  2018;5:180287
  53. Quantification of Total and Mutant Huntingtin Protein Levels in Biospecimens Using a Novel alphaLISA Assay.
    Authors: Baldo Et al.
    Eneuro  2018;5
  54. A Glial Signature and Wnt7 Signaling Regulate Glioma-Vascular Interactions and Tumor Microenvironment.
    Authors: Rakesh K Et al.
    Cancer Cell  2018;33:874-889.e7
  55. Exit from Naive Pluripotency Induces a Transient X Chromosome Inactivation-like State in Males.
    Authors: Sousa Et al.
    Cell Stem Cell  2018;22:919
  56. 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
  57. Specification of murine ground state pluripotent stem cells to regional neuronal populations.
    Authors: Alsanie
    Sci Rep  2017;7(1):16001
  58. Derivation of telencephalic oligodendrocyte progenitors from human pluripotent stem cells.
    Authors: Major Et al.
    Curr Protoc Stem Cell Biol  2017;39:1H.10.1
  59. Degree of tissue differentiation dictates susceptibility to BRAF-driven colorectal cancer.
    Authors: Tong
    Cell Rep  2017;21(13):3833
  60. Circadian networks in human embryonic stem cell-derived cardiomyocytes.
    Authors: Dierickx Et al.
    EMBO Rep  2017;18:1199
  61. 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
  62. 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
  63. 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
  64. Generating high-purity cardiac and endothelial derivatives from patterned mesoderm using humanpluripotent stem cells
    Authors: Palpant Et al.
    Nature Protocols  2016;12:15
  65. 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
  66. 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
  67. 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
  68. Plasticity of Hopx(+) type I alveolar cells to regenerate type II cells in the lung.
    Authors: Jain Et al.
    Nat Commun  2015;6:6727
  69. 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
  70. A balance of positive and negative regulators determines the pace of the segmentation clock.
    Authors: Wiedermann Et al.
    Elife  2015;4
  71. 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
  72. Neural cells play an inhibitory role in pancreatic differentiation of pluripotent stem cells.
    Authors: Nakashima Et al.
    Genes Cells  2015;20:1028
  73. Prostaglandin E2 promotes MYCN non-amplified neuroblastoma cell survival via β-catenin stabilization.
    Authors: Jansen Et al.
    Blood  2015;19:210
  74. 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
  75. 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
  76. 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
  77. A zebrafish chemical suppressor screening identifies small molecule inhibitors of the Wnt/β-catenin pathway.
    Authors: Nishiya Et al.
    Chem Biol  2014;21:530
  78. Critical roles of p53 in epithelial-mesenchymal transition and metastasis of hepatocellular carcinoma cells.
    Authors: Wang Et al.
    Genome Biol  2013;8:e72846
  79. 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
  80. WNT3 is a biomarker capable of predicting the definitive endoderm differentiation potential of hESCs.
    Authors: Jiang Et al.
    Stem Cell Reports  2013;1:46
  81. Transmembrane protein 88: a Wnt regulatory protein that specifies cardiomyocyte development.
    Authors: Palpant Et al.
    Development  2013;140:3799
  82. BMP-mediated specification of the erythroid lineage suppresses endothelial development in blood island precursors.
    Authors: Myers and Krieg
    Blood  2013;122:3929
  83. 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
  84. 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
  85. Axin2 as regulatory and therapeutic target in newborn brain injury and remyelination.
    Authors: Fancy Et al.
    Nat Neurosci  2011;14:1009
  86. NKG2D receptor regulates human effector T-cell cytokine production.
    Authors: Barber and Sentman
    Cell Res  2011;117:6571

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