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

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.

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CAS 番号 : 284028-89-3

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カスタマーレビュー

Based on 190 publication(s) in Google Scholar

Other Forms of XAV-939:

Top Publications Citing Use of Products

顧客検証

2D/3D Cell Culture and Differentiation
IF
WB

    XAV-939 purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2023 Jun 7;15(6):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: Nature. 2022 Jan;601(7894):600-605.  [Abstract]

    Upon exposure to lysophosphatidic acid (LPA) (a Hippo pathway inhibitor), A83-01 (an inhibitor of TGFβ family receptors) and PD0325901 (an ERK inhibitor) in a chemically defined medium containing the STAT activator leukaemia inhibitory factor (LIF) and Y-27632 (a ROCK inhibitor) (10 µM, 7 days),blastocyst-like structures formed efficiently from naive PSCs.

    XAV-939 purchased from MedChemExpress. Usage Cited in: Nature. 2022 Jan;601(7894):600-605.  [Abstract]

    Upon exposure to lysophosphatidic acid (LPA) (a Hippo pathway inhibitor), A83-01 (an inhibitor of TGFβ family receptors) and PD0325901 (an ERK inhibitor) in a chemically defined medium containing the STAT activator leukaemia inhibitory factor (LIF) and Y-27632 (a ROCK inhibitor) (10 µM, 7 days), blastocyst-like structures formed efficiently from naive PSCs. trophectoderm (TE) cell analogues (identified as GATA2+GATA3+CDX2+TROP2+) formed, proliferated, and established adherens junctions (marked by CDH1), apical-basal polarity (indicated by aPKC) and tight junctions (marked by ZO-1).

    XAV-939 purchased from MedChemExpress. Usage Cited in: Ecotoxicol Environ Saf. 2023 Jan 1:249:114410.  [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: 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: 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: 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: 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: 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.

    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).
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    • 参考文献

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    製品説明

    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)

    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    12.3 μM
    Compound: XAV939
    Growth inhibition of human A549 cells after 72 hrs by MTT assay
    Growth inhibition of human A549 cells after 72 hrs by MTT assay
    [PMID: 29934219]
    COLO 320DM GI50
    17 μM
    Compound: XAV939
    Antiproliferative activity against human COLO320DM cells assessed as inhibition of cell growth measured after 4 days by CellTiter-Glo assay
    Antiproliferative activity against human COLO320DM cells assessed as inhibition of cell growth measured after 4 days by CellTiter-Glo assay
    [PMID: 30883102]
    DLD-1 IC50
    0.707 μM
    Compound: 1, XAV-939
    Inhibition of tankyrase in human DLD1 cells assessed as reduction in Wnt activity after 24 hrs by TCF-luciferase reporter gene assay
    Inhibition of tankyrase in human DLD1 cells assessed as reduction in Wnt activity after 24 hrs by TCF-luciferase reporter gene assay
    [PMID: 25299683]
    HEK-293T IC50
    51 nM
    Compound: 2, XAV939
    Inhibition of beta-casein-dependent canonical Wnt3 pathway in human HEK293T cells by luciferase reporter gene assay
    Inhibition of beta-casein-dependent canonical Wnt3 pathway in human HEK293T cells by luciferase reporter gene assay
    [PMID: 22191557]
    HEK293 IC50
    0.078 μM
    Compound: 1, XAV939
    Inhibition of mouse Wnt3A signaling in human HEK293 cells after 1 day by super top flash luciferase reporter gene assay
    Inhibition of mouse Wnt3A signaling in human HEK293 cells after 1 day by super top flash luciferase reporter gene assay
    [PMID: 22260203]
    HEK293 IC50
    0.078 μM
    Compound: 1, XAV939
    Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin
    Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin
    [PMID: 23844574]
    HEK293 IC50
    0.078 μM
    Compound: 1, XAV939
    Inhibition of Wnt signaling in human HEK293 cells assessed as inhibition of forskolin-induced cAMP response element activation by STF luciferase reporter gene assay
    Inhibition of Wnt signaling in human HEK293 cells assessed as inhibition of forskolin-induced cAMP response element activation by STF luciferase reporter gene assay
    [PMID: 23879431]
    HEK293 IC50
    272 μM
    Compound: 3, XAV939
    Inhibition of Tankyrase in human HEK293 cells assessed as inhibition of Wnt pathway by Wnt3a-induced STF assay
    Inhibition of Tankyrase in human HEK293 cells assessed as inhibition of Wnt pathway by Wnt3a-induced STF assay
    [PMID: 23316926]
    SW480 EC50
    0.371 μM
    Compound: 1, XAV939
    Stabilization of Axin2 in human SW480 cells after 24 hrs by sandwich ELISA
    Stabilization of Axin2 in human SW480 cells after 24 hrs by sandwich ELISA
    [PMID: 22260203]
    SW480 GI50
    > 50 μM
    Compound: XAV939
    Growth inhibition of human SW480 cells by Cell-titer-fluor reagent based assay
    Growth inhibition of human SW480 cells by Cell-titer-fluor reagent based assay
    [PMID: 31769984]
    Sf21 IC50
    0.0053 μM
    Compound: 1, XAV939
    Inhibition of N-terminal GST-tagged TNKS2 (unknown origin) expressed in baculovirus infected sf21 cells after 60 mins by LC-MS analysis
    Inhibition of N-terminal GST-tagged TNKS2 (unknown origin) expressed in baculovirus infected sf21 cells after 60 mins by LC-MS analysis
    [PMID: 23879431]
    Sf21 IC50
    17 nM
    Compound: 5; XAV939
    Inhibition of N-terminal GST-tagged human TNKS-2 (849 to 1166 residues) expressed in in insect sf21 cells preincubated for 2 hrs followed by substrate addition measured after 30 mins
    Inhibition of N-terminal GST-tagged human TNKS-2 (849 to 1166 residues) expressed in in insect sf21 cells preincubated for 2 hrs followed by substrate addition measured after 30 mins
    [PMID: 27163581]
    Sf9 IC50
    2.1 nM
    Compound: XAV939
    Inhibition of human N-terminal GST-tagged TNKS2 (667 to 1166 residues) expressed in baculovirus infected Sf9 insect cells using histone as substrate measured after 1 hr by horseradish peroxidase-coupled chemiluminescence assay
    Inhibition of human N-terminal GST-tagged TNKS2 (667 to 1166 residues) expressed in baculovirus infected Sf9 insect cells using histone as substrate measured after 1 hr by horseradish peroxidase-coupled chemiluminescence assay
    [PMID: 31042381]
    Sf9 IC50
    4.2 nM
    Compound: XAV939
    Inhibition of human N-terminal GST-tagged TNKS1 (1001 to 1327 residues) expressed in baculovirus infected Sf9 insect cells using histone as substrate measured after 1 hr by horseradish peroxidase-coupled chemiluminescence assay
    Inhibition of human N-terminal GST-tagged TNKS1 (1001 to 1327 residues) expressed in baculovirus infected Sf9 insect cells using histone as substrate measured after 1 hr by horseradish peroxidase-coupled chemiluminescence assay
    [PMID: 31042381]
    体外実験

    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.
    体内実験

    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.

    分子量

    312.31

    分子式

    C14H11F3N2OS

    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

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

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    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)

    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
    10 mM 0.3202 mL 1.6010 mL 3.2019 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 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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    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.
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    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.
    純度とドキュメンテーション

    純度: 99.91%

    参考文献

    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 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. 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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    一般には略語で表示されます:C1V1 = C2V2

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    • Do most proteins show cross-species activity?

      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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    Inquiry Information

    製品名:
    XAV-939
    製品番号:
    HY-15147
    数量:
    MCE 日本正規代理店: