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Submit ReviewXAV 939
GMP Version Available:
XAV 939
说明： Potent tankyrase inhibitor
别名： XAV939 Wnt Signaling Inhibitor
化学名： 3,5,7,8-Tetrahydro-2-[4-(trifluoromethyl)phenyl]-4H-thiopyrano[4,3-d]pyrimidin-4-one
纯度： ≥98% (HPLC)
生物活性 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.
化合物库 for XAV 939
XAV 939 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Epigenetics Library and Tocriscreen Stem Cell Library. 了解 Tocris 化合物库的更多信息。
技术数据 for XAV 939
| 分子量 | 312.31 |
| 公式 | C14H11F3N2OS |
| 储存 | Store at RT |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for XAV 939
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 6.25 | 20 |
制备储备液 for XAV 939
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for XAV 939
参考文献 for XAV 939
参考文献是支持产品生物活性的出版物。
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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关键词: 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 篇 XAV 939 的引用文献
引用文献是使用了 Tocris 产品的出版物。 XAV 939 的部分引用包括：
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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
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Palpant et al (2016) Generating high-purity cardiac and endothelial derivatives from patterned mesoderm using humanpluripotent stem cells Nature Protocols 12 15 PMID: 27906170
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
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Yoon et al (2019) Reliability of human cortical organoid generati Nat Methods 16 75 PMID: 30573846
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Dierickx et al (2017) Circadian networks in human embryonic stem cell-derived cardiomyocytes. EMBO Rep 18 1199 PMID: 28536247
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 (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
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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
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
Alsanie (2017) Specification of murine ground state pluripotent stem cells to regional neuronal populations. Sci Rep 7 16001 PMID: 29167563
Barber and Sentman (2011) NKG2D receptor regulates human effector T-cell cytokine production. Cell Res 117 6571 PMID: 21518928
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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
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
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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
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
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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
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
Wolf et al (2022) Amniogenesis occurs in two independent waves in primates. Cell Stem Cell 29 744-759.e6 PMID: 35439430
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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
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Wnt signaling inhibitor.
By
Kishor Pant on 05/22/2019
分析类型： In Vitro
种属： Human
细胞系/组织： HuCCt1 and H69
XAV 393 inhibits the B-catenin expression in cancer cells in-vitro at 500nM.
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