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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Cited by 83 Publications

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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 MmTQT4lv[XOnIFHzd4F6 NFjJbZQyQC55NTFOwG0> M3Hz[FYxKG2rbh?= MlL5SG1UVw>? MmTpTY5pcWKrdHnvckBw\iCQLYTldo1qdmGuIFfTWE11[WepZXSgWG5MWzJiZYjwdoV{e2WmIIfpeIghUUN3MDDv[kAxNjByNUOg{txO M4n2dFI{QDd7NEOx
HEK293T M3Lx[GZ2dmO2aX;uJGF{e2G7 NYPXWYZCTE2VTx?= NHzIVWRKdmirYnn0bY9vKG:oIGfueEB{cWewYXzpcoch[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBnd3K|a3;sbY4ucW6mdXPl[EBkSU2SIILld5BwdnOnIHXs[Y1mdnRiYXP0bZZifGmxbjD3bZRpKEmFNUCgc4YhOC5yN{ig{txO MkjzNlM5Pzl2M{G=
HEK293T NX[wcoVXTnWwY4Tpc44hSXO|YYm= M{PQWVExKM7:TR?= NE\2T|VFVVOR M1rGOWlvcGmkaYTpc44hd2ZiYnX0ZU1k[XOnaX6t[IVx\W6mZX70JINidm:waXPhcEBYdnR|IIDheIh4[Xlid3n0bEBKSzVyIH;mJFAvODVzIN88US=> MUiyNlE6OTV3Nx?=
HEK293T M1rCR2Z2dmO2aX;uJGF{e2G7 NFLEOoMzPCCq NF\FUVVFVVOR NXvsfHV4UW6qaXLpeIlwdiCxZjDtc5V{\SCZboSzRUB{cWewYXzpcochf2m2aDDJR|UxKG:oIECuNFc5KM7:TR?= M1L5ZlIzOjZyMkCz
SW480 NHTpNnFHfW6ldHnvckBCe3OjeR?= NYjnVGd[OTBizszN MViyOEBp MYjEUXNQ M4X4U3N1[WKrbHn6ZZRqd25ib3[gRZhqdjJid3n0bEBGSzVyIH;mJFAvOzdzIN88US=> M3P2UVIzOjZyMkCz
HEK293T NUTiWIJtTnWwY4Tpc44hSXO|YYm= NH\vOm42OCEQvF2= MVrEUXNQ MUXIZZMhdm9iRX\m[YN1KG:wIH\vdpNsd2yrbj3pcoR2[2WmIHPBUXAhe2mpbnHsbY5oKGmwIHj1cYFvKEiHS{K5N3Qh[2WubIOgZ49mgHC{ZYPzbY5oKEOURR?= NHm4cmkzOjJ4MEKwNy=>
IEC-6 Mmn2SpVv[3Srb36gRZN{[Xl? M1P1e|YhcA>? M4O1UWFvfGGpb37pd5Qh[WO2aY\peJkh[XRiQnX0ZU1k[XSnbnnuM3RETiCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKFewdD2zZU1qdmS3Y3XkJIF5cW5{IHX4dJJme3Orb36ge4l1cCCLQ{WwJI9nKDBwNkSg{txO Ml6yNlQxPjB2OEm=
IEC-6 M3[3Z2Z2dmO2aX;uJGF{e2G7 NV76U4s3PiCq MVfBcpRi\2:waYP0JIFkfGm4aYT5JIF1KEKndHGtZ4F1\W6rbj;UR2Yh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBYdnRvM3GtbY5lfWOnZDDs[5I2KGW6cILld5Nqd25id3n0bEBKSzVyIH;mJFIvQSEQvF2= NY\XcWIzOjRyNkC0PFk>
DLD1 M1;nSWZ2dmO2aX;uJGF{e2G7 M2\MPVIxKM7:TR?= Mn;nNlQhcA>? M2HnemROW09? NGDUVVdKdmirYnn0bY9vKG:oIIThcot6emG|ZTDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIGTDSk1l\XCnbnTlcpQhfHKjboPjdolxfGmxbnHsJIFkfGm4aYT5 NYH4PI1pOjR3Mke3PVI>
DLD1 NXn6UplCS3m2b4TvfIlkKEG|c3H5 M{\ZcVIxKM7:TR?= M{LDe|ExKGR? M3n5b2ROW09? NVr0SGRDS3m2b4TvfIlkcXS7IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;u NX\C[5dlOjR3Mke3PVI>
VERO NIC3U3RHfW6ldHnvckBCe3OjeR?= MmrENlUh|ryP MVXEUXNQ MYDEbZN1fXKkZYOgVGFTKGKnbISgd5lvfGinc3nzMEBi\m[nY4TpcochfGinIHHjeIlvKGO7dH;zb4Vt\XSxbjygZ4VtdCC|aHHw[UBidmRiY3XscEBi\Ginc3nvci=> NVHUZ|U{OjV|M{K4OFU>
HeLa NWS2doc4TnWwY4Tpc44hSXO|YYm= MUCxNEDPxE1? MoPiOFghcA>? MYPS[YR2[3Srb36gc4Yh[3m2b4DsZZNucWNiZHnzeJJq[nW2aX;uJIFv\CCwdXPs[YFzKHS{YX7zcI9k[XSrb36gc4Yh|rJvY3H0[Y5qdg>? M{GwZlI2ODZzNEm5
SiHa MoHvSpVv[3Srb36gRZN{[Xl? NXHEUoRnOTBizszN NWH5N3pqPDhiaB?= MXzS[YR2[3Srb36gc4Yh[3m2b4DsZZNucWNiZHnzeJJq[nW2aX;uJIFv\CCwdXPs[YFzKHS{YX7zcI9k[XSrb36gc4Yh|rJvY3H0[Y5qdg>? NGH3b3AzPTB4MUS5PS=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
β-catenin / E-cadherin / N-cadherin; 

PubMed: 31060551     


Western blot of the β-catenin, E-cadherin and N-cadherin proteins after treatment with the β-catenin inhibitor XAV-939 (100 μM) for 48 h in the indicated cells. β-Tubulin was used as a loading control. 

β-catenin / c-Myc / cyclin D1 / E-cadherin / N-cadherin / Vimentin ; 

PubMed: 28177909     


In the fibulin-4 shRNA-infected cells, Wnt signaling pathway inhibitor XAV-939 could significantly inhibit the Wnt/β-catenin pathway and EMT, both of which were activated by fibulin-4 knockdown.

31060551 28177909
Immunofluorescence
β-catenin / E-cadherin ; 

PubMed: 31060551     


Immunofluorescence of subcellular β-catenin and E-cadherin localization after treatment with the β-catenin inhibitor XAV-939 (100 μM) for 48 h in the indicated cells.

Actin / PAR; 

PubMed: 25332845     


(A)-(C) Actin (red), (D)-(F) PAR (green), (G)-(I) merge. (A, D, G) control, (B, E, H) 3 mM EGTA, (C, F, I) 25 µM XAV 939. Bar: 25 µm.

Hes1 / β-catenin / p-STAT3; 

PubMed: 25061499     


Immunofluorescent staining of Hes1 in HeLa and SiHa cells without (N) and with (L) 8 µM L685,458 treatment for 48h. Immunofluorescent staining of β-catenin in HeLa and SiHa cells without (N) and with (XAV) 10 μM XAV-939 treatment for 48h. Immunofluorescent staining of p-STAT3 in HeLa and SiHa cells without (N) and with (AG) 80 μM AG490 treatment for 48h.

31060551 25332845 25061499

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 (38.42 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+corn oil
For best results, use promptly after mixing.
1mg/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

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    I want to inject XAV 939 (Cat # S1180) into mice through I.P. and just wonder what kind of solvent/solution I can use for this.

  • Answer:

    S1180 XAV-939 can be dissolved in 4% DMSO+corn oil at 1 mg/ml as a clear solution. When preparing the solution, please dissolve the compound in DMSO clearly first. You can sonicate and warm it in water bath at about 45 degree to help dissolving. Then dilute with corn oil.

Wnt/beta-catenin Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID