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 NET6VpJMcW6jc3WgRZN{[Xl? MVyxPE44PSEQvF2= NFznPJg3OCCvaX6= NGXybWNFVVOR MU\Jcohq[mm2aX;uJI9nKE5vdHXycYlv[WxiR2PUMZRi\2enZDDUUmtUOiCneIDy[ZN{\WRid3n0bEBKSzVyIH;mJFAvODB3MzFOwG0> MXyyN|g4QTR|MR?=
HEK293T MoXrSpVv[3Srb36gRZN{[Xl? M2\lUGROW09? NIHjV5JKdmirYnn0bY9vKG:oIGfueEB{cWewYXzpcoch[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBnd3K|a3;sbY4ucW6mdXPl[EBkSU2SIILld5BwdnOnIHXs[Y1mdnRiYXP0bZZifGmxbjD3bZRpKEmFNUCgc4YhOC5yN{ig{txO NHXnd|AzOzh5OUSzNS=>
HEK293T NITuOoNHfW6ldHnvckBCe3OjeR?= MoTJNVAh|ryP NUPXSnJUTE2VTx?= M{Tve2lvcGmkaYTpc44hd2ZiYnX0ZU1k[XOnaX6t[IVx\W6mZX70JINidm:waXPhcEBYdnR|IIDheIh4[Xlid3n0bEBKSzVyIH;mJFAvODVzIN88US=> M2nQUFIzOTlzNUW3
HEK293T MYrGeY5kfGmxbjDBd5NigQ>? NEnORYozPCCq M{LMOGROW09? MVnJcohq[mm2aX;uJI9nKG2xdYPlJHdvfDODIIPp[45idGmwZzD3bZRpKEmFNUCgc4YhOC5yN{ig{txO M2LvOlIzOjZyMkCz
SW480 NGrrcVJHfW6ldHnvckBCe3OjeR?= MlrONVAh|ryP MnOwNlQhcA>? M{X0cGROW09? MkPUV5Ri[mmuaYrheIlwdiCxZjDBfIlvOiC5aYToJGVEPTBib3[gNE4{PzFizszN NFnK[mIzOjJ4MEKwNy=>
HEK293T NF3Bd3JHfW6ldHnvckBCe3OjeR?= MYK1NEDPxE1? M2HGNGROW09? NVrwNJBFUGG|IH7vJGVn\mWldDDvckBnd3K|a3;sbY4ucW6mdXPl[EBkSU2SIIPp[45idGmwZzDpckBpfW2jbjDISWszQTOWIHPlcIx{KGOxZYjwdoV{e2mwZzDDVmU> NV\1S|BiOjJ{NkCyNFM>
IEC-6 M1fMRmZ2dmO2aX;uJGF{e2G7 NV7ucVRIPiCq NVjnVYY6SW62YXfvcol{fCCjY4Tpeol1gSCjdDDC[ZRiNWOjdHXubY4wXEOIIHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiV370MVNiNWmwZIXj[YQh[XirbkKg[ZhxemW|c3nvckB4cXSqIFnDOVAhd2ZiMD62OEDPxE1? M37Pb|I1ODZyNEi5
IEC-6 NE\CZ|BHfW6ldHnvckBCe3OjeR?= M2DGNVYhcA>? M2LVW2FvfGGpb37pd5Qh[WO2aY\peJkh[XRiQnX0ZU1k[XSnbnnuM3RETiCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKFewdD2zZU1qdmS3Y3XkJIxoejViZYjwdoV{e2mxbjD3bZRpKEmFNUCgc4YhOi57IN88US=> NGjMW4szPDB4MES4PS=>
DLD1 MnTOSpVv[3Srb36gRZN{[Xl? M3nTdVIxKM7:TR?= MYGyOEBp MnHSSG1UVw>? MYXJcohq[mm2aX;uJI9nKHSjbnv5doF{\SCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKFSFRj3k[ZBmdmSnboSgeJJidnOlcnnweIlwdmGuIHHjeIl3cXS7 NUPQfGo2OjR3Mke3PVI>
DLD1 NXL4[3JpS3m2b4TvfIlkKEG|c3H5 NE[wb4kzOCEQvF2= NHW4Z|UyOCCm M1\Kb2ROW09? MmfuR5l1d3SxeHnjbZR6KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:w M{jSOlI1PTJ5N{my
VERO M2qzTGZ2dmO2aX;uJGF{e2G7 MVyyOUDPxE1? NFTxfnZFVVOR Ml[xSIl{fHW{YnXzJHBCWiCkZXz0JJN6dnSqZYPpd{wh[W[oZXP0bY5oKHSqZTDhZ5RqdiCleYTvd4tmdGW2b36sJINmdGxic3jhdIUh[W6mIHPlcIwh[WSqZYPpc44> MV2yOVM{Ojh2NR?=
HeLa MXPGeY5kfGmxbjDBd5NigQ>? NWDPU2c{OTBizszN NIrDTFc1QCCq MYjS[YR2[3Srb36gc4Yh[3m2b4DsZZNucWNiZHnzeJJq[nW2aX;uJIFv\CCwdXPs[YFzKHS{YX7zcI9k[XSrb36gc4Yh|rJvY3H0[Y5qdg>? NIL3TnIzPTB4MUS5PS=>
SiHa NV:0TlE3TnWwY4Tpc44hSXO|YYm= NEXWSpkyOCEQvF2= NYTHXXhlPDhiaB?= MnHSVoVlfWO2aX;uJI9nKGO7dH;wcIF{dWmlIHTpd5RzcWK3dHnvckBidmRiboXjcIVieiC2cnHud4xw[2G2aX;uJI9nKM7{LXPheIVvcW5? NYTn[JV6OjVyNkG0PVk>

... Click to View More Cell Line Experimental Data

Protocol

Cell Research:[1]
+ Expand
  • 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 slightly soluble or insoluble
Ethanol slightly soluble or insoluble
In vivo Add solvents individually and in order:
30% PEG 400+0.5% Tween 80+5% Propylene glycol
30mg/mL

* 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