XAV 939

Tocris Bioscience a Bio-Techne Brand

Catalog # 3748

Citations (41)

(1)

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Key Product Details

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)
Molecular Weight:	312.31

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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

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.

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 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 for XAV 939

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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	160.10 mL
1 mM	3.20 mL	16.01 mL	32.02 mL
2 mM	1.60 mL	8.00 mL	16.01 mL
10 mM	0.32 mL	1.60 mL	3.20 mL

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References for XAV 939

References are publications that support the biological activity of the product.

Wang Cardiac induction of embryonic stem cells by a small molecule inhibitor of Wnt/β-catenin signaling. ACS Chem. Biol. 2010 PMID: 21077691
Huang Tankyrase inhibition stabilizes axin and antagonizes wnt signalling. Nature 2009 PMID: 19759537
Adler Inhibiting wnt signaling. Sci.Signal.

Citations for XAV 939 (41)

Showing 1 - 10 of 41 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for XAV 939 include:

Yoon et al. (2019) Reliability of human cortical organoid generati Nat Methods. 16:75
PMID: 30573846
Rostovskaya et al. (2019) Capacitation of human na�ve 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
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
Whitehead (2018) Heparanase attenuates axon degeneration following sciatic nerve transection. Sci Rep. 8(1):5219
PMID: 29581478
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
Pereira et al. (2018) Polysome profiling followed by RNA-seq of cardiac differentiation stages in hESCs. Sci Data. 5:180287
PMID: 30512016
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(1):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(28):E5599
PMID: 28655839
Tong (2017) Degree of tissue differentiation dictates susceptibility to BRAF-driven colorectal cancer. Cell Rep. 21(13):3833
PMID: 29281831
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
Dierickx et al. (2017) Circadian networks in human embryonic stem cell-derived cardiomyocytes. EMBO Rep. 18:1199
PMID: 28536247
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
Palpant et al. (2016) Generating high-purity cardiac and endothelial derivatives from patterned mesoderm using humanpluripotent stem cells Nature Protocols. 12:15
PMID: 27906170
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
Xu et al. (2016) Wnt/β-catenin signaling promotes self-renewal and inhibits the primed state transition in na�ve human embryonic stem cells. Proc Natl Acad Sci U S A. 113:E6382
PMID: 27698112
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
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
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
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
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. (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
Wang et al. (2013) Critical roles of p53 in epithelial-mesenchymal transition and metastasis of hepatocellular carcinoma cells. Genome Biol. 8:e72846
PMID: 24023784
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
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
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
Fancy et al. (2011) Axin2 as regulatory and therapeutic target in newborn brain injury and remyelination. Nat Neurosci. 14:1009
PMID: 21706018
Barber and Sentman (2011) NKG2D receptor regulates human effector T-cell cytokine production. Cell Res. 117:6571
PMID: 21518928

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Wnt signaling inhibitor

Name: Kishor Pant

Species: Human

Assay Type: In Vitro

Cell Line/Tissue: HuCCt1 and H69

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

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