XAV 939

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Cat.No. 3748 - XAV 939 | C14H11F3N2OS | CAS No. 284028-89-3
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% (HPLC)
Datasheet
Citations (29)
Reviews
Protocols (1)
Literature

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.

Compound Libraries

XAV 939 is also offered as part of the Tocriscreen Plus and Tocriscreen Stem Cell Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 6.25 20

Preparing Stock Solutions

The following data is based on the product molecular weight 312.31. Batch specific molecular weights may vary from batch to batch due to solvent 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

Certificate of Analysis / Product Datasheet
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References

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


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View all Tankyrase Inhibitors

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, Beta-catenin, Poly(ADP-ribose), Polymerase, Stem, Cell, Signaling, Tankyrase, 3748, Tocris Bioscience

29 Citations for XAV 939

Citations are publications that use Tocris products. Selected citations for XAV 939 include:

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

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

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

Whitehead (2018) Heparanase attenuates axon degeneration following sciatic nerve transection. Sci Rep 8 5219 PMID: 29581478

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

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

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

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

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

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

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

Palpant et al (2016) Generating high-purity cardiac and endothelial derivatives from patterned mesoderm using humanpluripotent stem cells Nature Protocols 12 15 PMID: 27906170


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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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Cancer

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