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XAV-939

Catalog No. T1878   CAS 284028-89-3
Synonyms: XAV939, NVP-XAV939

XAV-939 (NVP-XAV939) is a Tankyrase (TNKS) inhibitor that inhibits TNKS1 and TNKS2 (IC50=11/4 nM). XAV-939 selectively inhibits Wnt/β-catenin-mediated transcription.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
XAV-939 Chemical Structure
XAV-939, CAS 284028-89-3
Pack Size Availability Price/USD Quantity
5 mg In stock $ 48.00
10 mg In stock $ 59.00
25 mg In stock $ 111.00
50 mg In stock $ 179.00
100 mg In stock $ 276.00
200 mg In stock $ 490.00
1 mL * 10 mM (in DMSO) In stock $ 54.00
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Purity: 99.04%
Purity: 98.9%
Purity: 98%
Purity: 97.47%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description XAV-939 (NVP-XAV939) is a Tankyrase (TNKS) inhibitor that inhibits TNKS1 and TNKS2 (IC50=11/4 nM). XAV-939 selectively inhibits Wnt/β-catenin-mediated transcription.
Targets&IC50 TNKS1:11 nM (cell free), TNKS2:4 nM (cell free)
In vitro METHODS: Human colorectal cancer cells SW480 were treated with XAV-939 (1 µM) for 16 h. The expression levels of target proteins were detected by Western Blot.
RESULTS: XAV-939 decreased the abundance of β-catenin and increased the abundance of axin and p-β-catenin in SW480 cells. [1]
METHODS: Normal human epidermal keratinocytes NHEK were treated with XAV-939 (10-50 µM) and rhIL-6 (50 ng/mL) for 24 h, and the number of target cells was detected by APC BrdU flow kit.
RESULTS: XAV-939 largely inhibited the over-proliferation of NHEK. [2]
In vivo METHODS: To investigate the in vivo function of Wnt signaling, XAV-939 (1 mg/mL, 100 μL, 10% DMSO/90% 0.9% NaCl) was administered intraperitoneally to an IMQ-induced psoriasis mouse model once daily for seven days.
RESULTS: Administration of XAV-939 resulted in a significant reduction of IMQ-induced epidermal hyperplasia and dermal inflammatory infiltration in mice. XAV-939 administration significantly reduced the infiltration of F4/80+ macrophages and CD3+ T cells in IMQ-induced inflammatory dermal lesions.Wnt signaling is critical for IMQ-mediated epidermal hyperplasia. [2]
METHODS: To assay antitumor activity in vivo, paclitaxel (10 mg/kg) and XAV-939 (10 mg/kg) were injected intraperitoneally twice weekly for four weeks into BALB/c nude mice harboring human mammary carcinoma tumor MDA-MB-231.
RESULTS: The combination of paclitaxel and XAV-939 effectively inhibited the growth of mammary tumors compared with control and each single treatment. [3]
Cell Research XAV939, the recently identified small molecule shown to specifically inhibit PARP activity of tankyrase 1 (and tankyrase 2 at higher concentrations), was used here at much lower concentrations than 3-AB. The tankyrase specific inhibitor XAV939 was solubilized in DMSO at 55°C to a stock concentration of 10mM, which was diluted to a working concentration of 100μM; final concentrations of 0.5μM or 1μM were well within the concentration parameters suggested for cell culture experiments to inhibit tankyrase specifically. Cultures were maintained under these conditions for the duration of the designated time course. Controls were exposed to DMSO alone. Following treatment, cells were lysed and prepared for western blot analysis. Tankyrase 1 and DNA-PKcs protein levels were normalized to the β-actin loading controls and quantified [1].
Animal Research XAV-939, a selective inhibitor of tankyrase (TNKS)-1 and TNKS-2, was injected i.p., at a dose of 1 mg/ml, once a day for seven consecutive days of IMQ treatment (injection volume 100 μl). Control mice were injected with 100 μl 10% DMSO/90% 0.9% NaCl, the solvent for XAV-939 [3].
Synonyms XAV939, NVP-XAV939
Molecular Weight 312.31
Formula C14H11F3N2OS
CAS No. 284028-89-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 12.5 mg/mL (40.02 mM)

TargetMolReferences and Literature

1. Huang SM, et al. Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling. Nature. 2009 Oct 1;461(7264):614-20. 2. Bai J, et al. Epigenetic downregulation of SFRP4 contributes to epidermal hyperplasia in psoriasis. J Immunol. 2015 May 1;194(9):4185-98. 3. Shetti D, et al. Low Dose of Paclitaxel Combined with XAV939 Attenuates Metastasis, Angiogenesis and Growth in Breast Cancer by Suppressing Wnt Signaling. Cells. 2019 Aug 14;8(8):892. 4. Geng W, Guo X, Zhang L, et al. Resveratrol inhibits proliferation, migration and invasion of multiple myeloma cells via NEAT1-mediated Wnt/β-catenin signaling pathway[J]. Biomedicine & Pharmacotherapy. 2018 Nov;107:484-494.

TargetMolCitations

1. Wu M, Zhang X, Zhang W, et al. Cancer Stem Cell Regulated Phenotypic Plasticity Protects Metastasized Cancer Cells from Ferroptosis. Nature Communications. 2022, 13(1): 1-16. 2. Liu X, Xie P, Hao N, et al. HIF-1–regulated expression of calreticulin promotes breast tumorigenesis and progression through Wnt/β-catenin pathway activation. Proceedings of the National Academy of Sciences. 2021, 118(44) 3. Geng W, Guo X, Zhang L, et al. Resveratrol inhibits proliferation, migration and invasion of multiple myeloma cells via NEAT1-mediated Wnt/β-catenin signaling pathway,Resveratrol inhibits proliferation, migration and invasion of multiple myeloma cells via NEAT1-mediated Wnt/β-catenin signaling pathway. Biomedicine & Pharmacotherapy. 2018 Nov;107:484-494. 4. Li X Y, Shi J, Zhao W, et al. Wnt16 from decidual stromal cells regulates HTR8/SVneo trophoblastic cell function via Akt/β-catenin pathway. Reproduction. 2022, 1(aop). 5. Zhou M, He J, Li Y, et al.N6-methyladenosine modification of REG1α facilitates colorectal cancer progression via β-catenin/MYC/LDHA axis mediated glycolytic reprogramming.Cell Death & Disease.2023, 14(8): 557. 6. Wu M, Zhang X, Zhang W, et al.Paracrine secretion of IL8 by breast cancer stem cells promotes therapeutic resistance and metastasis of the bulk tumor cells.Cell Communication and Signaling.2023, 21(1): 1-17. 7. Sun R, Luo Y, Liu J, et al.Carbon Dioxide Fractional Laser Treatment Induces Lgr5+ Stem Cell Activation and Hair Regrowth Through the Canonical Wnt/β-Catenin Pathway.Aesthetic Plastic Surgery.2023: 1-15. 8. Yan L, Wu M, Wang T, et al.Breast Cancer Stem Cells Secrete MIF to Mediate Tumor Metabolic Reprogramming that Drives Immune Evasion.Cancer Research.2024

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Reprogramming Compound Library Epigenetics Compound Library Bioactive Lipid Compound Library Anti-Colorectal Cancer Compound Library Anti-Cancer Metabolism Compound Library Anti-Pancreatic Cancer Compound Library Stem Cell Differentiation Compound Library Cytoskeletal Signaling Pathway Compound Library Anti-Ovarian Cancer Compound Library

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Keywords

XAV-939 284028-89-3 Chromatin/Epigenetic Cytoskeletal Signaling DNA Damage/DNA Repair Stem Cells PARP Wnt/beta-catenin poly ADP ribose polymerase XAV939 Inhibitor XAV 939 NVP-XAV-939 NVP-XAV939 β-catenin NVP-XAV 939 inhibit Beta catenin inhibitor

 

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