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Submit ReviewXAV 939
GMP Version Available:
XAV 939
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% (HPLC)
Biological Activity for XAV 939
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 for XAV 939
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.
Compound Libraries for XAV 939
XAV 939 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Epigenetics Library and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.
Technical Data for XAV 939
| M. Wt | 312.31 |
| Formula | C14H11F3N2OS |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 284028-89-3 |
| PubChem ID | 2726824 |
| InChI Key | KLGQSVMIPOVQAX-UHFFFAOYSA-N |
| Smiles | OC1=C(CSCC2)C2=NC(C3=CC=C(C(F)(F)F)C=C3)=N1 |
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.
Solubility Data for XAV 939
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 6.25 | 20 |
Preparing Stock Solutions for XAV 939
The following data is based on the product molecular weight 312.31. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 16.01 mL | 80.05 mL | 160.1 mL |
| 1 mM | 3.2 mL | 16.01 mL | 32.02 mL |
| 2 mM | 1.6 mL | 8 mL | 16.01 mL |
| 10 mM | 0.32 mL | 1.6 mL | 3.2 mL |
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Product Datasheets for XAV 939
References for XAV 939
References are publications that support the biological activity of the product.
Huang et al (2009) Tankyrase inhibition stabilizes axin and antagonizes wnt signalling. Nature 461 614 PMID: 19759537
Adler (2009) Inhibiting wnt signaling. Sci.Signal. 91
Wang et al (2010) Cardiac induction of embryonic stem cells by a small molecule inhibitor of Wnt/β-catenin signaling. ACS Chem. Biol. 6 192 PMID: 21077691
If you know of a relevant reference for XAV 939, please let us know.
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Keywords: XAV 939, XAV 939 supplier, XAV939, wnt, signalling, signaling, b-catenin, β-catenin, beta-catenin, axin, TNKS1, TNKS2, tankyrase, inhibitors, inhibits, PARP, poly(ADP-ribose), polymerases, cardiogenesis, cardiomyocyte, differentiation, Wnt, Signaling, Inhibitor, Beta-catenin, Poly(ADP-ribose), Polymerase, Stem, Cell, Tankyrase, Cardiomyocyte, Cells, Organoids, 3748, Tocris Bioscience
86 Citations for XAV 939
Citations are publications that use Tocris products. Selected citations for XAV 939 include:
Pecha et al (2019) Human iPS cell-derived engineered heart tissue does not affect ventricular arrhythmias in a guinea pig cryo-injury model. Sci Rep 9 9831 PMID: 31285568
Tong (2017) Degree of tissue differentiation dictates susceptibility to BRAF-driven colorectal cancer. Cell Rep 21 3833 PMID: 29281831
Al-Dhfyan (2017) Aryl hydrocarbon receptor/cytochrome P450 1A1 pathway mediates breast cancer stem cells expansion through PTEN inhibition and β-Catenin and Akt activation. Mol Cancer 16 14 PMID: 28103884
Mallinger et al (2015) Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. J Med Chem 58 1717 PMID: 25680029
Nakashima et al (2015) Neural cells play an inhibitory role in pancreatic differentiation of pluripotent stem cells. Genes Cells 20 1028 PMID: 26514269
Hong et al (2015) β-catenin promotes regulatory T-cell responses in tumors by inducing vitamin A metabolism in dendritic cells. Cancer Res 75 656 PMID: 25568183
Palpant et al (2015) Cardiac development in zebrafish and human embryonic stem cells is inhibited by exposure to tobacco cigarettes and e-cigarettes. PLoS One 10 e0126259 PMID: 25978043
Jain et al (2015) Plasticity of Hopx(+) type I alveolar cells to regenerate type II cells in the lung. Nat Commun 6 6727 PMID: 25865356
Wiedermann et al (2015) A balance of positive and negative regulators determines the pace of the segmentation clock. Elife 4 PMID: 26357015
Gerbin et al (2015) Enhanced Electrical Integration of Engineered Human Myocardium via Intramyocardial versus Epicardial Delivery in Infarcted Rat Hearts. PLoS One 10 e0131446 PMID: 26161513
Yang et al (2012) WLS inhibits melanoma cell proliferation through the β-catenin signalling pathway and induces spontaneous metastasis. EMBO Mol Med 4 1294 PMID: 23129487
Rostovskaya et al (2019) Capacitation of human naïve pluripotent stem cells for multi-lineage differentiation. Development 146 PMID: 30944104
Bertero et al (2019) Dynamics of genome reorganization during human cardiogenesis reveal an RBM20-dependent splicing factory. Nat Commun 10 1538 PMID: 30948719
Stuart et al (2019) Distinct Molecular Trajectories Converge to Induce Naive Pluripotency. Cell Stem Cell 25 388 PMID: 31422912
Koopmans et al (2017) β-Catenin Directs Nuclear Factor-κB p65 Output via CREB-Binding Protein/p300 in Human Airway Smooth Muscle. Front Immunol 8 1086 PMID: 28943877
Marc et al (2019) Human SNORA31 variations impair cortical neuron-intrinsic immunity to HSV-1 and underlie herpes simplex encephalitis. Nat Med 25 1873-1884 PMID: 31806906
Juan Carlos et al (2019) Generation of Blastocyst-like Structures from Mouse Embryonic and Adult Cell Cultures. Cell 179 687-702.e18 PMID: 31626770
Ryan M et al (2019) Specification of positional identity in forebrain organoids. Nat Biotechnol 37 436-444 PMID: 30936566
Alejandro et al (2019) Generation of ERK-Independent Human and Non-Human Primate Pluripotent Stem Cells. Curr Protoc Stem Cell Biol 49 e85 PMID: 30995363
Pereira et al (2018) Polysome profiling followed by RNA-seq of cardiac differentiation stages in hESCs. Sci Data 5 180287 PMID: 30512016
Whitehead (2018) Heparanase attenuates axon degeneration following sciatic nerve transection. Sci Rep 8 5219 PMID: 29581478
Rakesh K et al (2018) A Glial Signature and Wnt7 Signaling Regulate Glioma-Vascular Interactions and Tumor Microenvironment. Cancer Cell 33 874-889.e7 PMID: 29681511
Palpant et al (2016) Generating high-purity cardiac and endothelial derivatives from patterned mesoderm using humanpluripotent stem cells Nature Protocols 12 15 PMID: 27906170
Nishiya et al (2014) A zebrafish chemical suppressor screening identifies small molecule inhibitors of the Wnt/β-catenin pathway. Chem Biol 21 530 PMID: 24684907
Wolf et al (2022) Amniogenesis occurs in two independent waves in primates. Cell Stem Cell 29 744-759.e6 PMID: 35439430
Wendy et al (2022) The human amniotic epithelium confers a bias to differentiate toward the neuroectoderm lineage in human embryonic stem cells. Elife 11 PMID: 35815953
Karoly et al (2022) Large-scale genome editing based on high-capacity adenovectors and CRISPR-Cas9 nucleases rescues full-length dystrophin synthesis in DMD muscle cells. Nucleic Acids Res 50 7761-7782 PMID: 35776127
Elisabeth et al (2022) Autophagy modulates cell fate decisions during lineage commitment. Autophagy 18 1915-1931 PMID: 34923909
Daniel H et al (2022) Dissecting the molecular basis of human interneuron migration in forebrain assembloids from Timothy syndrome. Cell Stem Cell 29 248-264.e7 PMID: 34990580
Dmitry et al (2022) Naïve-like pluripotency to pave the way for saving the northern white rhinoceros from extinction. Sci Rep 12 3100 PMID: 35260583
Arjun et al (2022) Cell type determination for cardiac differentiation occurs soon after seeding of human-induced pluripotent stem cells. Genome Biol 23 90 PMID: 35382863
Xiaolu et al (2022) A dual SHOX2:GFP; MYH6:mCherry knockin hESC reporter line for derivation of human SAN-like cells. iScience 25 104153 PMID: 35434558
Suho et al (2022) Alzheimer risk gene product Pyk2 suppresses tau phosphorylation and phenotypic effects of tauopathy. Mol Neurodegener 17 32 PMID: 35501917
Naoyuki et al (2022) Ivermectin represses Wnt/β-catenin signaling by binding to TELO2, a regulator of phosphatidylinositol 3-kinase-related kinases. iScience 25 103912 PMID: 35530256
Zhen et al (2022) A stem cell roadmap of ribosome heterogeneity reveals a function for RPL10A in mesoderm production. Nat Commun 13 5491 PMID: 36123354
Omer et al (2022) Engineering brain assembloids to interrogate human neural circuits. Nat Protoc 17 15-35 PMID: 34992269
Wolf et al (2022) 8C-like cells capture the human zygotic genome activation program in vitro. Cell Stem Cell 29 449-459.e6 PMID: 35216671
Jiuru et al (2022) A single cell transcriptional roadmap of human pacemaker cell differentiation. Elife 11 PMID: 36217819
Lars M et al (2022) Efficient Gene Expression in Human Stem Cell Derived-Cortical Organoids Using Adeno Associated Virus. Cells 11 PMID: 36291062
Yavuz et al (2022) STRAIGHT-IN enables high-throughput targeting of large DNA payloads in human pluripotent stem cells. Cell Rep Methods 2 100300 PMID: 36313798
Olivier et al (2022) Paraxial mesoderm organoids model development of human somites. Elife 11 PMID: 35088712
Gerald W et al (2022) Norepinephrine transporter defects lead to sympathetic hyperactivity in Familial Dysautonomia models. Nat Commun 13 7032 PMID: 36396637
Kerensa et al (2022) Use of standard U-bottom and V-bottom well plates to generate neuroepithelial embryoid bodies. PLoS One 17 e0262062 PMID: 35536781
Xu et al (2016) Wnt/β-catenin signaling promotes self-renewal and inhibits the primed state transition in naïve human embryonic stem cells. Proc Natl Acad Sci U S A 113 E6382 PMID: 27698112
Koopmans et al (2016) Selective targeting of CREB-binding protein/β-catenin inhibits growth of and extracellular matrix remodelling by airway smooth muscle. Br J Pharmacol 173 3327 PMID: 27629364
Jiang et al (2013) WNT3 is a biomarker capable of predicting the definitive endoderm differentiation potential of hESCs. Stem Cell Reports 1 46 PMID: 24052941
Myers and Krieg (2013) BMP-mediated specification of the erythroid lineage suppresses endothelial development in blood island precursors. Blood 122 3929 PMID: 24100450
Wu et al (2012) Differential modulation of the oligodendrocyte transcriptome by sonic hedgehog and bone morphogenetic protein 4 via opposing effects on histone acetylation. J Neurosci 32 6651 PMID: 22573687
Fancy et al (2011) Axin2 as regulatory and therapeutic target in newborn brain injury and remyelination. Nat Neurosci 14 1009 PMID: 21706018
Minal et al (2023) Differentiation of human induced pluripotent stem cells into cortical neural stem cells. Front Cell Dev Biol 10 1023340 PMID: 36684426
Mi-Hyeon et al (2023) Nicotinamide Mononucleotide Prevents Cisplatin-Induced Mitochondrial Defects in Cortical Neurons Derived from Human Induced Pluripotent Stem Cells. Brain Plast 8 143-152 PMID: 36721392
Shiyong et al (2023) Lipid droplet-associated lncRNA LIPTER preserves cardiac lipid metabolism. Nat Cell Biol PMID: 37264180
Yang et al (2020) GAS2 Promotes Cell Proliferation and Invasion and Suppresses Apoptosis in Pediatric T-Cell Acute Lymphoblastic Leukemia and Activates Wnt/β-Catenin Pathway. Onco Targets Ther 13 1099-1108 PMID: 32103979
Abraham J et al (2020) Human-iPSC-Derived Cardiac Stromal Cells Enhance Maturation in 3D Cardiac Microtissues and Reveal Non-cardiomyocyte Contributions to Heart Disease. Cell Stem Cell 26 862-879.e11 PMID: 32459996
Chris et al (2020) Variable expression and silencing of CRISPR-Cas9 targeted transgenes identifies the AAVS1 locus as not an entirely safe harbour. F1000Res 8 1911 PMID: 32789000
Benedicte et al (2020) Intraflagellar Transport Complex B Proteins Regulate the Hippo Effector Yap1 during Cardiogenesis. Cell Rep 32 107932 PMID: 32698004
Geoffrey et al (2020) Tissue-Specific Regulation of the Wnt/β-Catenin Pathway by PAGE4 Inhibition of Tankyrase. Cell Rep 32 107922 PMID: 32698014
Nadine et al (2020) Cell Type-Specific In Vitro Gene Expression Profiling of Stem Cell-Derived Neural Models. Cells 9 PMID: 32516938
Cheng-mao et al (2020) Norrin restores blood-retinal barrier properties after vascular endothelial growth factor-induced permeability. J Biol Chem 295 4647-4660 PMID: 32086377
Major et al (2017) Derivation of telencephalic oligodendrocyte progenitors from human pluripotent stem cells. Curr Protoc Stem Cell Biol 39 1H.10.1 PMID: 29081882
Szabo et al (2015) Statistically based splicing detection reveals neural enrichment and tissue-specific induction of circular RNA during human fetal development. Dis Model Mech 16 126 PMID: 26076956
Ma et al (2015) Downregulation of Wnt signaling by sonic hedgehog activation promotes repopulation of human tumor cell lines. J Cell Mol Med 8 385 PMID: 25713298
Jansen et al (2015) Prostaglandin E2 promotes MYCN non-amplified neuroblastoma cell survival via β-catenin stabilization. Blood 19 210 PMID: 25266063
Palpant et al (2013) Transmembrane protein 88: a Wnt regulatory protein that specifies cardiomyocyte development. Development 140 3799 PMID: 23924634
Sousa et al (2018) Exit from Naive Pluripotency Induces a Transient X Chromosome Inactivation-like State in Males. Cell Stem Cell 22 919 PMID: 29804891
Okamoto et al (2018) MERIT40-dependent recruitment of tankyrase to damaged DNA and its implication for cell sensitivity to DNA-damaging anticancer drugs. Oncotarget 9 35844 PMID: 30533199
Baldo et al (2018) Quantification of Total and Mutant Huntingtin Protein Levels in Biospecimens Using a Novel alphaLISA Assay. Eneuro 5 PMID: 30310861
Hoch et al (2015) MRT-92 inhibits Hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor. FASEB J 29 1817 PMID: 25636740
Jiang et al (2013) Histone H3K27me3 demethylases KDM6A and KDM6B modulate definitive endoderm differentiation from human ESCs by regulating WNT signaling pathway. ASN Neuro 23 122 PMID: 22907667
Wang et al (2013) Critical roles of p53 in epithelial-mesenchymal transition and metastasis of hepatocellular carcinoma cells. Genome Biol 8 e72846 PMID: 24023784
Sean P et al (2021) A comprehensive analysis of gene expression changes in a high replicate and open-source dataset of differentiating hiPSC-derived cardiomyocytes. Sci Rep 11 15845 PMID: 34349150
Arun et al (2021) Responsiveness to perturbations is a hallmark of transcription factors that maintain cell identity in vitro. Cell Syst 12 885-899.e8 PMID: 34352221
Joseph C et al (2021) Pathogenic LMNA variants disrupt cardiac lamina-chromatin interactions and de-repress alternative fate genes. Cell Stem Cell 28 938-954.e9 PMID: 33529599
Alison M et al (2021) ELAVL4, splicing, and glutamatergic dysfunction precede neuron loss in MAPT mutation cerebral organoids. Cell 184 4547-4563.e17 PMID: 34314701
Beth A et al (2021) Resolving cell state in iPSC-derived human neural samples with multiplexed fluorescence imaging. Commun Biol 4 786 PMID: 34168275
Viviana et al (2021) Generation, functional analysis and applications of isogenic three-dimensional self-aggregating cardiac microtissues from human pluripotent stem cells. Nat Protoc 16 2213-2256 PMID: 33772245
Insa S et al (2021) A Human 3D Cardiomyocyte Risk Model to Study the Cardiotoxic Influence of X-rays and Other Noxae in Adults. Cells 10 PMID: 34685588
Ling et al (2021) Commitment and oncogene-induced plasticity of human stem cell-derived pancreatic acinar and ductal organoids. Cell Stem Cell 28 1090-1104.e6 PMID: 33915081
Cecilia et al (2021) Mapping the temporal and spatial dynamics of the human endometrium in vivo and in vitro. Nat Genet 53 1698-1711 PMID: 34857954
Yang et al (2021) Urokinase-type plasminogen activator-mediated crosstalk between N-cadherin and β-Catenin promotes wound healing. J Cell Sci PMID: 33929542
Yang et al (2021) Urokinase-type plasminogen activator-mediated crosstalk between N-cadherin and β-catenin promotes wound healing. J Cell Sci 134 PMID: 34085693
Yoon et al (2019) Reliability of human cortical organoid generati Nat Methods 16 75 PMID: 30573846
Alsanie (2017) Specification of murine ground state pluripotent stem cells to regional neuronal populations. Sci Rep 7 16001 PMID: 29167563
Young (2017) The doublesex-related Dmrta2 safeguards neural progenitor maintenance involving transcriptional regulation of Hes1. Proc Natl Acad Sci U S A. 114 E5599 PMID: 28655839
Dierickx et al (2017) Circadian networks in human embryonic stem cell-derived cardiomyocytes. EMBO Rep 18 1199 PMID: 28536247
Barber and Sentman (2011) NKG2D receptor regulates human effector T-cell cytokine production. Cell Res 117 6571 PMID: 21518928
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Filter by:
Wnt signaling inhibitor.
By
Kishor Pant on 05/22/2019
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: HuCCt1 and H69
XAV 393 inhibits the B-catenin expression in cancer cells in-vitro at 500nM.
Protocols for XAV 939
The following protocol features additional information for the use of XAV 939 (Cat. No. 3748).
Literature in this Area
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