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

XAV-939 

Cat. No.: HY-15147 Purity: 98.04%
Handling Instructions

XAV-939 is a tankyrase (TNKS) inhibitor and an indirect inhibitor of Wnt/β-catenin signaling, with IC50s of 5 and 2 nM for TNKS1 and TNKS2, respectively.

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

XAV-939 Chemical Structure

XAV-939 Chemical Structure

CAS No. : 284028-89-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 72 In-stock
Estimated Time of Arrival: December 31
50 mg USD 216 In-stock
Estimated Time of Arrival: December 31
100 mg USD 336 In-stock
Estimated Time of Arrival: December 31
200 mg USD 600 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

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Customer Review

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

    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: Proc Natl Acad Sci U S A. 2016 Mar 29;113(13):E1898-906.

    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: Cell Physiol Biochem. 2016;39(1):360-70.

    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 MCE. Usage Cited in: Biochim Biophys Acta. 2016 Dec;1859(12):1527-1537.

    RVX208 increases CTGF and CYR61 expression and TAZ protein level in HCT116 cells.

    XAV-939 purchased from MCE. Usage Cited in: Biochim Biophys Acta. 2016 Dec;1859(12):1527-1537.

    JQ1 treatment decreases β-catenin levels in HCT116 cells, but increases TAZ protein. When cells reach confluence, they are serum-starved overnight and pretreated with DMSO or JQ1 (500 nM) for 1 hour, followed by growth medium (containing 10% serum) stimulation for 24 hours.

    XAV-939 purchased from MCE. Usage Cited in: Biomed Res Int. 2017;2017:1972608.

    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: Cell Death Dis. 2018 Jan 18;9(2):27.

    Overexpression PCDHGA9 induces GC cell apoptosis, cell cycle arrest, and autophagy. Western blot analysis determines that 10 μg/mL V-ZAD-FMK inhibits the activation of caspases.

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

    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: Anticancer Drugs. 2018 Mar;29(3):208-215.

    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: Anticancer Drugs. 2018 Mar;29(3):208-215.

    SUM159 sphere-forming cells are treated with Vismodegib (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: Front Pharmacol. 2018 Jun 21;9:660.

    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 (erlotinib), p38 MAPK (TAK-715), and Smad3 (SIS3) inhibitors and are followed by TWEAK stimulation.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    XAV-939 is a tankyrase (TNKS) inhibitor and an indirect inhibitor of Wnt/β-catenin signaling, with IC50s of 5 and 2 nM for TNKS1 and TNKS2, respectively.

    IC50 & Target

    IC50: 5 nM (TNKS1), 2 nM (TNKS2)[6]

    In Vitro

    XAV939 (1 μM) strongly inhibis STF activity in SW480 cells, Wnt3a-stimulated STF activity in HEK293 cells, but does not affect CRE, NF-κB or TGF-β luciferase reporters. XAV939 regulates axin levels through tankyrase inhibition in HEK293 cell[1]. XAV939 (0.5 μM, 1.0 μM) reduces DNA-PKcs protein levels 50% of the relative DMSO control in human lymphoblasts[2]. XAV939 induces a second wave of pro-cardiomyocyte gene expression as shown by increased Mesp1 and Isl1expression 2 to 4 days after Wnt inhibition, and by increased Nkx2.5 expression 4 to 6 days after XAV939 addition[3]. XAV-939 (10 nM) has a suppressive effect on elevated MMP-13 levels in both IL-1β-induced SW 1353 cells[4].

    In Vivo

    XAV-939 (3 mL, 10 nM) has a suppressive effect on elevated MMP-13 levels in the rat OA model[4]. XAV-939 (1 mg/mL, i.p.) ameliorates the psoriasiform skin disease induced by IMQ. XAV-939 results in a significant decrease in the IMQ-induced epidermal hyperplasia (indicated by acanthosis) and dermal inflammatory infiltrates in mice[5].

    Solvent & Solubility
    In Vitro: 

    DMSO : 21.5 mg/mL (68.84 mM; Need ultrasonic and warming)

    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.

      XAV-939 is dissolved in 0.9% sodium chloride[7].

    References
    Kinase Assay
    [1]

    To assess the effect of compounds on auto-PARsylation of TNKS, 1 μM GST fusion protein containing the SAM domain and the PARP domain of TNKS2 (a.a. 872-1166) is mixed with 5 μM biotin-NAD+ and 2 μM XAV939 or LDW643 at 30°C for 2.5 hours. Samples are resolved by SDS-PAGE and probed with streptavidin AlexaFluor680. To assess PARsylation of axin, recombinant full-length TNKS2 (expressed/purified as a N-terminal His-tagged protein in bacteria) is incubated with GST-axin 1 (1-280) in the presence of biotin-NAD+ with or without XAV939. The products are resolved and probed with Streptavidin-HRP and imaged using a AlphaInnotech imager. To assess the effect of XAV939, IWR-1-enod, IWR-1-exo, and ABT-888 on auto-PARsylation of TNKS2, His-tagged full-length TNKS2 is incubated with 5 μM biotin-NAD+ and 3 mM of indicated compounds. The products are resolved and probed with Streptavidin-HRP. LC/MS-based high throughput auto-PARsylation assays for PARP1, PARP2, TNKS1, and TNKS2 are setup to monitor the formation of nicotinamide (a by-product of the PARsylation reaction) in the presence of small molecule inhibitors.

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

    Cell Assay
    [4]

    Human SW 1353 chondrosarcoma cells are seeded in 96-well plates (1×104 cells/well) and are treated with Icariin (0, 5, 10, 20, 40, 80, or 100 μM). After 24 h, 20 μL MTT (5 mg/mL in PBS) is added to each well and plates are incubated at 37°C for another 4 h. Supernatants are then removed, and 150 μL dimethylsulfoxide is added to each well. After plates are shaken for 10 min, optical density values measured at 570 nm are recorded using an ELISA reader.

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

    Animal Administration
    [5]

    C57BL/6J mice are kept under specific pathogen-free conditions. XAV-939 is injected i.p., at a dose of 1 mg/mL, once a day for seven consecutive days of IMQ treatment (injection volume 100 mL). Control mice are injected with 100 mL 10% DMSO/90% 0.9% NaCl, the solvent for XAV-939. To ameliorate any suffering of mice observed throughout these experimental studies, they are euthanized by CO2 inhalation.

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

    References
    Molecular Weight

    312.31

    Formula

    C₁₄H₁₁F₃N₂OS

    CAS No.

    284028-89-3

    SMILES

    OC1=C2C(CCSC2)=NC(C3=CC=C(C=C3)C(F)(F)F)=N1

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 98.04%

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    Product Name:
    XAV-939
    Cat. No.:
    HY-15147
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    XAV-939

    Cat. No.: HY-15147