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

XAV-939 

Cat. No.: HY-15147 Purity: 99.91%
COA Handling Instructions

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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10 mM * 1 mL in DMSO USD 66 In-stock
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ready for reconstitution
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Solid
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10 mg USD 72 In-stock
50 mg USD 216 In-stock
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Customer Review

Based on 114 publication(s) in Google Scholar

Other Forms of XAV-939:

XAV-939 Related Antibodies

Top Publications Citing Use of Products

102 Publications Citing Use of MCE XAV-939

WB

    XAV-939 purchased from MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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.

    View All PARP Isoform Specific Products:

    View All Isoforms
    PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

    • 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].

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

    XAV-939 Related Antibodies

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    312.31

    Appearance

    Solid

    Formula

    C14H11F3N2OS
    CAS No.
    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 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 15.62 mg/mL (50.01 mM; ultrasonic and warming and heat to 60°C)

    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
    10 mM 0.3202 mL 1.6010 mL 3.2019 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.91%

    COA (247 KB) HNMR (273 KB) LCMS (264 KB) Elemental Analysis Report (106 KB)

    Handling Instructions (2659 KB)
    References
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    XAV-939 Related Classifications

    Help & FAQs
    • 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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    × = ×
    C1   V1   C2   V2

    Keywords:

    XAV-939284028-89-3XAV939XAV 939β-cateninPARPBeta cateninpoly ADP ribose polymeraseTankyraseTNKS1TNKS2hMSCsWnt signalingcancerfibrotic diseaselow bone formationInhibitorinhibitorinhibit

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