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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
41 Citations for XAV 939
Citations are publications that use Tocris products. Selected citations for XAV 939 include:
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
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
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
Tong (2017) Degree of tissue differentiation dictates susceptibility to BRAF-driven colorectal cancer. Cell Rep 21 3833 PMID: 29281831
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
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
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
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
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
Yoon et al (2019) Reliability of human cortical organoid generati Nat Methods 16 75 PMID: 30573846
Dierickx et al (2017) Circadian networks in human embryonic stem cell-derived cardiomyocytes. EMBO Rep 18 1199 PMID: 28536247
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
Barber and Sentman (2011) NKG2D receptor regulates human effector T-cell cytokine production. Cell Res 117 6571 PMID: 21518928
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
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
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
Palpant et al (2013) Transmembrane protein 88: a Wnt regulatory protein that specifies cardiomyocyte development. Development 140 3799 PMID: 23924634
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
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
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
Do you know of a great paper that uses XAV 939 from Tocris? Please let us know.
Reviews for XAV 939
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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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*Please note that Tocris will only send literature to established scientific business / institute addresses.
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