XAV-939

Catalog No.S1180 Synonyms: NVP-XAV939

XAV-939 Chemical Structure

Molecular Weight(MW): 312.31

XAV-939 selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β.

Size Price Stock Quantity  
In DMSO USD 91 In stock
USD 70 In stock
USD 170 In stock
USD 270 In stock
USD 770 In stock

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7 Customer Reviews

  • Fluorescence microscopy of pSuper or Cdo shRNA expressing P19 cells at ITS1 immunostained withβ-tubulin III antibodies. Size bar=100 um. P19/control or P19/Cdo shRNA cells were treated with DMSO or XAV939 in the differentiation medium for 72 h followed by immunostaining.

    Nat Commun 2014 5, 5455. XAV-939 purchased from Selleck.

    (I) Effect of XAV-939 on gefitinib efficacy in indicated NSCLC cells was detected by MTT assay (J) The indicated NSCLC cells were treated with gefitinib in the presence or absence of XAV-939, and then subjected to immunoblot analysis using the indicated antibodies. Data represent the mean ± SD of three independent experiments. *P < 0.05.

    cancer lett, 2016.. XAV-939 purchased from Selleck.

  • Images of the hfVM experiment described in C, comparing the effects of LIF-nano versus empty-nano at equivalent dilution (left panel) and XAV-nano versus empty-nano at equivalent dilution (right panel). Scale bars: 200 μm.

    Dis Model Mech 2014 7(10), 1193-203. XAV-939 purchased from Selleck.

    Pathology observation of mice liver sections stained with hematoxylin and eosin (H&E) and Masson (×200), and the levels of -SMA and Tmem88 were analyzed by immunohistochemistry (×200).

    Mol Immunol, 2016, 80:58-67. XAV-939 purchased from Selleck.

  • Cells plated at 2 x 104 in 24 multiwell with DMEM 10% FBS preconditioning 24 hrs (pretreatment without wnt) switch medium from 2% HS + WNT 100 ng/ml

    Dr. Marco Quarta of Stanford University. XAV-939 purchased from Selleck.

     

    Fig. 1.  Canonical Wnt Signaling Inhibits Prostatic Bud Number Similar to TCDD. E14.5 male UGSs were cultured for 4 days in media containing 10 nM DHT with either vehicle 1 nM TCDD; recombinant DKK1 + DKK2 (500 ng/ml each); or 10 μM XAV-939 to inhibit canonical Wnt signaling. Buds were visualized by performing IHC specific for ecadherin, an epithelium marker (green).  The number of prostatic buds was determined by confocal microscopy. Yellow arrowheads indicate areas where buds are present. U indicates urethra.  Results are mean ±SE for at least four litter-independent samples per treatment. Asterisk indicates a significant decrease compared to control p < 0.05.

    XAV-939 purchased from Selleck.

  • XAV-939 purchased from Selleck.

Purity & Quality Control

Choose Selective Wnt/beta-catenin Inhibitors

Biological Activity

Description XAV-939 selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β.
Targets
TNKS2 [1]
(Cell-free assay)
TNKS1 [1]
(Cell-free assay)
4 nM 11 nM
In vitro

XAV-939 specifically inhibits tankyrase PARP activity. XAV-939 dramatically decreases DNA-PKcs protein levels, confirming the critical role of tankyrase poly-ADP-ribosylation activity in maintaining stability of the DNA-PKcs protein. The greatest reduction of DNA-PKcs protein levels (< 25% relative expression compared to DMSO treated controls) occurs at 12 hours with 1.0 μM XAV-939 exposure. Treatment of human lymphoblasts with 1.0 μM XAV-939 results in marked elevation of tankyrase 1 levels. [1] XAV-939 is axin stabilizing agent. XAV-939 stimulates beta-catenin degradation by stabilizing axin, the concentration-limiting component of the destruction complex. XAV-939 stabilizes axin by blocking the poly-ADP-ribosylating enzymes tankyrase 1 and tankyrase 2. Both tankyrase isoforms interact with a highly conserved domain of axin and stimulate its degradation through the ubiquitin-proteasome pathway. XAV-939 deregulates the Wnt/b-catenin pathway which has been implicated in many cancers. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf-21 MVLLbY5ie2ViQYPzZZk> M3n3TVE5Njd3IN88US=> MlzBOlAhdWmw MoD0SG1UVw>? NX\wbHozUW6qaXLpeIlwdiCxZjDOMZRmem2rbnHsJGdUXC22YXfn[YQhXE6NU{Kg[ZhxemW|c3XkJJdqfGhiSVO1NEBw\iByLkCwOVMh|ryP M{LLZ|I{QDd7NEOx
HEK293T NHrYcZBHfW6ldHnvckBCe3OjeR?= M4\wPGROW09? NILuXpNKdmirYnn0bY9vKG:oIGfueEB{cWewYXzpcoch[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBnd3K|a3;sbY4ucW6mdXPl[EBkSU2SIILld5BwdnOnIHXs[Y1mdnRiYXP0bZZifGmxbjD3bZRpKEmFNUCgc4YhOC5yN{ig{txO NWXkT5p6OjN6N{m0N|E>
HEK293T NY\LTGw5TnWwY4Tpc44hSXO|YYm= MVmxNEDPxE1? M3rXZ2ROW09? NVnXO|d4UW6qaXLpeIlwdiCxZjDi[ZRiNWOjc3Xpck1l\XCnbnTlcpQh[2Gwb37pZ4FtKFewdEOgdIF1cHejeTD3bZRpKEmFNUCgc4YhOC5yNUGg{txO MlnzNlIyQTF3NUe=
HEK293T NF7QOVdHfW6ldHnvckBCe3OjeR?= NY\PTJQ6OjRiaB?= NGnyfJlFVVOR NFPybVZKdmirYnn0bY9vKG:oIH3veZNmKFewdEPBJJNq\26jbHnu[{B4cXSqIFnDOVAhd2ZiMD6wO|gh|ryP NUPUTFd6OjJ{NkCyNFM>
SW480 M3e5R2Z2dmO2aX;uJGF{e2G7 M4XzZlExKM7:TR?= MXiyOEBp MUXEUXNQ NIXEVJVUfGGkaXzpfoF1cW:wIH;mJGF5cW5{IIfpeIghTUN3MDDv[kAxNjN5MTFOwG0> Ml2xNlIzPjB{MEO=
HEK293T M2nY[GZ2dmO2aX;uJGF{e2G7 MXu1NEDPxE1? MorqSG1UVw>? MmLYTIF{KG6xIFXm[oVkfCCxbjDmc5J{c2:uaX6tbY5lfWOnZDDjRW1RKHOrZ37hcIlv\yCrbjDoeY1idiCKRVuyPVNVKGOnbHzzJINw\XiycnXzd4lv\yCFUlW= NVjOeJZiOjJ{NkCyNFM>
IEC-6 MXrGeY5kfGmxbjDBd5NigQ>? M4DoelYhcA>? NULIeHdtSW62YXfvcol{fCCjY4Tpeol1gSCjdDDC[ZRiNWOjdHXubY4wXEOIIHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiV370MVNiNWmwZIXj[YQh[XirbkKg[ZhxemW|c3nvckB4cXSqIFnDOVAhd2ZiMD62OEDPxE1? NHv2PWczPDB4MES4PS=>
IEC-6 NX\6eXRjTnWwY4Tpc44hSXO|YYm= M{LjZ|YhcA>? NYq4RVJzSW62YXfvcol{fCCjY4Tpeol1gSCjdDDC[ZRiNWOjdHXubY4wXEOIIHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiV370MVNiNWmwZIXj[YQhdGe{NTDlfJBz\XO|aX;uJJdqfGhiSVO1NEBw\iB{Lkmg{txO MnqyNlQxPjB2OEm=
DLD1 MXXGeY5kfGmxbjDBd5NigQ>? MkDENlAh|ryP M1S2XlI1KGh? MV3EUXNQ NFvMSGNKdmirYnn0bY9vKG:oIIThcot6emG|ZTDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIGTDSk1l\XCnbnTlcpQhfHKjboPjdolxfGmxbnHsJIFkfGm4aYT5 M4DsRlI1PTJ5N{my
DLD1 NIO1WHVEgXSxdH;4bYMhSXO|YYm= NEWwemkzOCEQvF2= NWXVfG9rOTBiZB?= MXrEUXNQ NFXxRoREgXSxdH;4bYNqfHliYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36= MXGyOFUzPzd7Mh?=
VERO Ml:3SpVv[3Srb36gRZN{[Xl? NXP6XmRbOjVizszN NW\yNFJpTE2VTx?= MoLXSIl{fHW{YnXzJHBCWiCkZXz0JJN6dnSqZYPpd{wh[W[oZXP0bY5oKHSqZTDhZ5RqdiCleYTvd4tmdGW2b36sJINmdGxic3jhdIUh[W6mIHPlcIwh[WSqZYPpc44> NYrwRoxUOjV|M{K4OFU>
HeLa M3zLRWZ2dmO2aX;uJGF{e2G7 NFHrZmUyOCEQvF2= Ml:4OFghcA>? NIC3TlBT\WS3Y4Tpc44hd2ZiY4n0c5Bt[XOvaXOg[Il{fHKrYoX0bY9vKGGwZDDueYNt\WG{IITyZY5{dG:lYYTpc44hd2ZizsKtZ4F1\W6rbh?= M1zjNlI2ODZzNEm5
SiHa NGTlOmNHfW6ldHnvckBCe3OjeR?= NX3id5RjOTBizszN NGKzdYI1QCCq MnHBVoVlfWO2aX;uJI9nKGO7dH;wcIF{dWmlIHTpd5RzcWK3dHnvckBidmRiboXjcIVieiC2cnHud4xw[2G2aX;uJI9nKM7{LXPheIVvcW5? Mn\WNlUxPjF2OUm=

... Click to View More Cell Line Experimental Data

Protocol

Cell Research:[1]
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  • Cell lines: WTK1 lymphoblasts
  • Concentrations: 1.0 μM
  • Incubation Time: 8 hours
  • Method: XAV-939 is solubilized in DMSO at 55 °C to make a 10 mM stock solution which may be diluted later to a working concentration of 100 μM. WTK1 lymphoblasts treated with either DMSO or 1.0 μM XAV-939 for 8 hours are loaded into independent wells of a 4-20% gradient SDS-PAGE every 2 hours over the course of 6 hours. At each time point, DMSO and XAV-939 samples are loaded into wells immediately adjacent to the prior time point. The corresponding load times at 0, 2 and 4 hours results in total run times of 2, 4 and 6 hours respectively. The gel is analyzed via western blot for DNA-PKcs following completion of the final run time and is quantified after normalization to actin loading controls.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 12 mg/mL warmed (38.42 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% PEG 400+0.5% Tween 80+5% Propylene glycol 30mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 312.31
Formula

C14H11F3N2OS

CAS No. 284028-89-3
Storage powder
in solvent
Synonyms NVP-XAV939

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID