1. Stem Cell/Wnt Epigenetics Cell Cycle/DNA Damage
  2. β-catenin PARP
  3. XAV-939

XAV-939 est un tankyrase inhibiteur puissant qui cible la signalisation Wnt/β-caténine. XAV-939 stabilise l'axine par inhiber les tankyrase 1 et tankyrase 2 (IC50s de 5 et 2 nM, respectivement), il stimule ainsi la dégradation de la β-caténine. XAV939 se lie étroitement aux domaines catalytiques (PARP) de TNKS1 et TNKS2 (Kds de 99 et 93 nM, respectivement).

XAV-939 ist ein potenter tankyrase, der auf die Wnt/β-catenin signaling abzielt. XAV-939 stabilisiert Axin durch Hemmung von tankyrase 1 und tankyrase 2 (IC50 von 5 bzw. 2 nM) und stimuliert dadurch den Abbau von β-Catenin. XAV-939 bindet eng an die katalytischen (PARP-)Domänen von TNKS1 und TNKS2 (Kds von 99 bzw. 93 nM).

XAV-939 is a Tankyrase inhibitor. XAV-939 has inhibitory activity for TNKS1 and TNKS2 with IC50 values of 5 nM and 2 nM, respectively. XAV-939 also is an enhancer of osteoblastic differentiation of hMSCs. XAV-939 can be used for the research of conditions associated with activated Wnt signaling, such as cancer, fibrotic diseases and conditions associated with low bone formation.

For research use only. We do not sell to patients.

XAV-939 Chemical Structure

XAV-939 Chemical Structure

CAS No. : 284028-89-3

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Customer Review

Based on 128 publication(s) in Google Scholar

Other Forms of XAV-939:

Top Publications Citing Use of Products

116 Publications Citing Use of MCE XAV-939

WB

    XAV-939 purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2023 Apr 20;e17101.  [Abstract]

    XAV939 (20 μM; 3 days) restores the expression of Homer1, PSD95, and GluR1 in Shank3 knockout (KO) human neurons.

    XAV-939 purchased from MedChemExpress. Usage Cited in: Ecotoxicol Environ Saf. 2022 Dec 12;249:114410.  [Abstract]

    XAV-939 (5 μM) significantly decreases the expression level of β-catenin in A549 cells.

    XAV-939 purchased from MedChemExpress. Usage Cited in: Am J Physiol Renal Physiol. 2020 Sep 1;319(3):F458-F468.  [Abstract]

    Representative Western blot showing FN protein abundance in HMCs cultured in media containing NG or HG in the absence or presence of liraglutide (100 nM) or DMSO (1:1000) or XAV-939 (5 μM) for 24 h.

    XAV-939 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Jan 18;9(2):27.  [Abstract]

    The cellular locations of β-catenin are detected by western blot. GAPDH, Histone H3, and ATP1A1 are used to normalize protein expression in total lysates and nuclear and membrane fractions, respectively. SGC-7901 cells with PCDHGA9 overexpression or vector control cells are grown in media with or without 10 μg/mL inhibitor of β-catenin (XAV-939).

    XAV-939 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Jun 21;9:660.  [Abstract]

    By Western blotting, the α-SMA and palladin proteins are determined in cells that are pretreated with NF-κB (JSH-23), Wnt/β-catenin (XAV939), EGFR (CP-358774), p38 MAPK (TAK-715), and Smad3 (SIS3) inhibitors and are followed by TWEAK stimulation.

    XAV-939 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 10;503(3):2061-2067.  [Abstract]

    Western blot analysis and alizarin red staining of hDFSCs transfected by EZH2-siRNA and treated by XAV-939. DMSO is used as a vehicle control.

    XAV-939 purchased from MedChemExpress. Usage Cited in: Anticancer Drugs. 2018 Mar;29(3):208-215.  [Abstract]

    SUM159 sphere-forming cells are treated with GDC-0449 (15 μM), a Smoothened (Smo) inhibitor for 7 days, and the protein expression levels of breast cancer stem cells (CSCs) play markers are detected by western blotting.

    XAV-939 purchased from MedChemExpress. Usage Cited in: Anticancer Drugs. 2018 Mar;29(3):208-215.  [Abstract]

    SUM159 sphereforming cells are treated with 15 μM XAV-939 for 7 days, and the protein expression levels of breast cancer stem cells (CSCs) markers are detected by western blotting.

    XAV-939 purchased from MedChemExpress. Usage Cited in: Biomed Res Int. 2017;2017:1972608.  [Abstract]

    To investigate the roles of β-catenin, XAV939 (β-catenin inhibitor) was added to MNT group. Total protein is used to observe the expression of Nrf2 and LC3.

    XAV-939 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2016 Mar 29;113(13):E1898-906.  [Abstract]

    Analysis of the in vitro role of the Wnt/β–catenin pathway in the regulation of AQP2 expression in response to sPRR-His treatment. Effect of XAV on sPRR-His-induced AQP2 expression (n = 6 per group).

    XAV-939 purchased from MedChemExpress. Usage Cited in: Comp Biochem Phys B. 2016 Jan;191:155-62.  [Abstract]

    The protein expression of Wnt10b and p-GSK-3β is significantly induced by LiCl treatment (A and B). Nevertheless, XAV939 treatment significantly inhibits the protein expression of p-GSK-3β (B). Moreover, the protein expression of p-β-catenin is significantly inhibited by LiCl treatment, but significantly induced by XAV939 treatment (C).

    XAV-939 purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2016;39(1):360-70.  [Abstract]

    EGF upregulates the expression of follicle-regulatory genes via Wnt/β-catenin signaling pathway. (A) The mRNA and (B, C) the protein levels of Survivin, Msx2 and SGK3 in the ORS cells with EGF treatment/overexpression and/or XAV-939 treatment.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    XAV-939 is a Tankyrase inhibitor. XAV-939 has inhibitory activity for TNKS1 and TNKS2 with IC50 values of 5 nM and 2 nM, respectively. XAV-939 also is an enhancer of osteoblastic differentiation of hMSCs. XAV-939 can be used for the research of conditions associated with activated Wnt signaling, such as cancer, fibrotic diseases and conditions associated with low bone formation[1][2][3].

    IC50 & Target[6]

    TNKS2

    2 nM (IC50)

    TNKS1

    5 nM (IC50)

    ARTD2

    479 nM (IC50)

    ARTD1

    5500 nM (IC50)

    In Vitro

    XAV-939 has activity against TNKS1 and TNKS2 with IC50 values of 5 nM and 2 nM, respectively[1].
    XAV-939 (0.3-30 μM; 3 or 10 days) enhances osteoblast differentiation of hBMSCs[2].
    XAV-939 (3 μM) promotes osteoblast differentiation of hMSCs via accumulation of SH3BP2[2].
    XAV-939 (3 μM; 10 days) upregulates the expression of OPG and downregulates the expression of RANKL in hBMSCs during osteoblast differentiation[2].
    XAV-939 suppresses Wnt/β-catenin signaling and promotes SFRP3 and SFRP4 expression[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Viability Assay[2]

    Cell Line: hMSC-TERT cell line
    Concentration: 0.3, 3, and 30 μM
    Incubation Time: 3 days
    Result: Showed no significant effect on proliferation at day 1, 2, and 3 at dose of 0.3 and 3 μM but inhibited hMSCs cell proliferation on day 3 at dose of 30 μM.

    Apoptosis Analysis[2]

    Cell Line: hMSC-TERT cell line
    Concentration: 3 µM
    Incubation Time: 3 days
    Result: Showed a minute percentage of cell death (apoptosis and necrosis) in the XAV-939-treated hBMSC

    RT-PCR[2]

    Cell Line: hMSC-TERT cell line
    Concentration: 3 µM
    Incubation Time: 10 days
    Result: Upregulated gene expression of osteoblast-associated gene markers including: ALP, COL1A1, RUNX2, and OC.
    In Vivo

    XAV-939 rescues mechanical stress-induced cartilage degeneration in vivo[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight

    312.31

    Formula

    C14H11F3N2OS

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C1C(CSCC2)=C2N=C(C3=CC=C(C(F)(F)F)C=C3)N1

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 15.62 mg/mL (50.01 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.2019 mL 16.0097 mL 32.0195 mL
    5 mM 0.6404 mL 3.2019 mL 6.4039 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 1.56 mg/mL (5.00 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1.56 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (15.6 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 1.56 mg/mL (5.00 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1.56 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (15.6 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 5 mg/mL (16.01 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

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    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
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    %
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.91%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.2019 mL 16.0097 mL 32.0195 mL 80.0487 mL
    5 mM 0.6404 mL 3.2019 mL 6.4039 mL 16.0097 mL
    10 mM 0.3202 mL 1.6010 mL 3.2019 mL 8.0049 mL
    15 mM 0.2135 mL 1.0673 mL 2.1346 mL 5.3366 mL
    20 mM 0.1601 mL 0.8005 mL 1.6010 mL 4.0024 mL
    25 mM 0.1281 mL 0.6404 mL 1.2808 mL 3.2019 mL
    30 mM 0.1067 mL 0.5337 mL 1.0673 mL 2.6683 mL
    40 mM 0.0800 mL 0.4002 mL 0.8005 mL 2.0012 mL
    50 mM 0.0640 mL 0.3202 mL 0.6404 mL 1.6010 mL
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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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