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XAV-939

Catalog No. T1878   CAS 284028-89-3
Synonyms: poly ADP ribose polymerase, PARP, Inhibitor, β-catenin, NVP-XAV939, XAV939, inhibit, Beta catenin, XAV-939, XAV 939

XAV-939 shows the selective inhibition against Wnt/β-catenin-mediated transcription by tankyrase1/2 inhibition (IC50: 11/4 nM in cell-free assays).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
XAV-939, CAS 284028-89-3
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Purity: 98%
Biological Description
Chemical Properties
Storage & Solubility Information
Description XAV-939 shows the selective inhibition against Wnt/β-catenin-mediated transcription by tankyrase1/2 inhibition (IC50: 11/4 nM in cell-free assays).
Targets&IC50 TNKS1:11 nM (cell free), TNKS2:4 nM (cell free)
In vitro Examination of various treatment times (2, 5, 8, 12, 18, 24 and 48 hr) and XAV939 concentrations (0.1, 0.5 or 1.0 μM) revealed a significant reduction of DNA-PKcs protein levels by 8 hours with exposures of either 0.5 μM or 1.0 μM XAV939 [1]. XAV939 blocks TNKS binding at 0.1 μM and blocks PARP1/2 binding at 1 μM. XAV939 binds tightly to the catalytic (PARP) domains of TNKS1 and TNKS2 (Kd = 0.099 and 0.093 μM, respectively) [2].
In vivo In contrast to vehicle control (VC), administration of XAV-939 resulted in a significant decrease in the IMQ-induced epidermal hyperplasia (indicated by acanthosis) and dermal inflammatory infiltrates in mice. XAV-939 administration remarkably decreased the infiltration of F4/80+ macrophages and CD3+ T cells in inflamed skin lesions induced by IMQ. Furthermore, reduced neutrophilic infiltrates in microabscesses were observed in the lesional skin treated with XAV-939 compared with VC [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 poly ADP ribose polymerase, PARP, Inhibitor, β-catenin, NVP-XAV939, XAV939, inhibit, Beta catenin, XAV-939, XAV 939
Molecular Weight 312.31
Formula C14H11F3N2OS
CAS No. 284028-89-3

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 6.3 mg/mL (20 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Dregalla RC, et al. Regulatory roles of tankyrase 1 at telomeres and in DNA repair: suppression of T-SCE and stabilization of DNA-PKcs. Aging (Albany NY). 2010 Oct;2(10):691-708. 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. Huang SM, et al. Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling. Nature. 2009 Oct 1;461(7264):614-620. 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. Bai J, et al. Epigenetic downregulation of SFRP4 contributes to epidermal hyperplasia in psoriasis. J Immunol. 2015 May 1;194(9):4185-98. doi: 10.4049/jimmunol.1403196. Epub 2015 Mar 30. 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. 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. 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).

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Compound Library Anti-Cancer Metabolism Compound Library Anti-Obesity Compound Library Inhibitor Library DNA Damage & Repair Compound Library Wnt/Hedgehog/Notch Compound Library Fluorochemical Library Anti-Cancer Active Compound Library Anti-Breast Cancer Compound Library Stem Cell Differentiation Compound Library

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