XAV-939

Catalog No.S1180 Synonyms: NVP-XAV939

For research use only.

XAV-939 (NVP-XAV939) 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.

XAV-939 Chemical Structure

CAS No. 284028-89-3

Selleck's XAV-939 has been cited by 293 publications

Purity & Quality Control

Choose Selective PARP Inhibitors

Other PARP Products

Biological Activity

Description XAV-939 (NVP-XAV939) 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 MnTXT4lv[XOnIFHzd4F6 M4PaSVE5Njd3IN88US=> M{OyTlYxKG2rbh?= MkjNSG1UVw>? MX\Jcohq[mm2aX;uJI9nKE5vdHXycYlv[WxiR2PUMZRi\2enZDDUUmtUOiCneIDy[ZN{\WRid3n0bEBKSzVyIH;mJFAvODB3MzFOwG0> MmDTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6N{m0N|EoRjJ|OEe5OFMyRC:jPh?=
HEK293T NX7zZ3FCTnWwY4Tpc44hSXO|YYm= MUfEUXNQ NYLGdpZ5UW6qaXLpeIlwdiCxZjDXcpQhe2mpbnHsbY5oKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh\m:{c3vvcIlvNWmwZIXj[YQh[0GPUDDy[ZNxd26|ZTDlcIVu\W62IHHjeIl3[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEe4JO69VQ>? MorYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6N{m0N|EoRjJ|OEe5OFMyRC:jPh?=
HEK293T NIHSPWxHfW6ldHnvckBCe3OjeR?= Ml;ZNVAh|ryP M{nqTWROW09? NUe3Zo9yUW6qaXLpeIlwdiCxZjDi[ZRiNWOjc3Xpck1l\XCnbnTlcpQh[2Gwb37pZ4FtKFewdEOgdIF1cHejeTD3bZRpKEmFNUCgc4YhOC5yNUGg{txO M{TDOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MUmxOVU4Lz5{MkG5NVU2PzxxYU6=
HEK293T NEPEOHlHfW6ldHnvckBCe3OjeR?= NYfkRocyOjRiaB?= MXzEUXNQ NFfwR5ZKdmirYnn0bY9vKG:oIH3veZNmKFewdEPBJJNq\26jbHnu[{B4cXSqIFnDOVAhd2ZiMD6wO|gh|ryP MkDYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{NkCyNFMoRjJ{Mk[wNlA{RC:jPh?=
SW480 NXrPWYtiTnWwY4Tpc44hSXO|YYm= M2jMe|ExKM7:TR?= MnHjNlQhcA>? MY\EUXNQ M4nZ[nN1[WKrbHn6ZZRqd25ib3[gRZhqdjJid3n0bEBGSzVyIH;mJFAvOzdzIN88US=> Ml;OQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{NkCyNFMoRjJ{Mk[wNlA{RC:jPh?=
HEK293T MWHGeY5kfGmxbjDBd5NigQ>? MUm1NEDPxE1? M1PaPGROW09? M17RVmhieyCwbzDF[oZm[3Rib36g[o9ze2uxbHnuMYlv\HWlZXSgZ2FOWCC|aXfuZYxqdmdiaX6gbJVu[W5iSFXLNlk{XCClZXzsd{Bkd2W6cILld5NqdmdiQ2LF M33TcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{Mk[wNlA{Lz5{MkK2NFIxOzxxYU6=
IEC-6 NU\SdpM2TnWwY4Tpc44hSXO|YYm= NIPCT5U3KGh? NGH1NWhCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IFLleIEu[2G2ZX7pck9VS0ZiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCZboStN4EucW6mdXPl[EBigGmwMjDlfJBz\XO|aX;uJJdqfGhiSVO1NEBw\iByLk[0JO69VQ>? M17BcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2ME[wOFg6Lz5{NEC2NFQ5QTxxYU6=
IEC-6 M3\HfmZ2dmO2aX;uJGF{e2G7 M{jKTlYhcA>? NE\UemNCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IFLleIEu[2G2ZX7pck9VS0ZiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCZboStN4EucW6mdXPl[EBt\3J3IHX4dJJme3Orb36ge4l1cCCLQ{WwJI9nKDJwOTFOwG0> MlP2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNkC0PFkoRjJ2ME[wOFg6RC:jPh?=
DLD1 MWDGeY5kfGmxbjDBd5NigQ>? MXWyNEDPxE1? MWSyOEBp MkTpSG1UVw>? NH6zc5JKdmirYnn0bY9vKG:oIIThcot6emG|ZTDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIGTDSk1l\XCnbnTlcpQhfHKjboPjdolxfGmxbnHsJIFkfGm4aYT5 NEPFW5A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEWyO|c6Oid-MkS1Nlc4QTJ:L3G+
DLD1 NEPZU2hEgXSxdH;4bYMhSXO|YYm= M1jIV|IxKM7:TR?= M4fEbVExKGR? NXHJS29GTE2VTx?= NX\3cXBSS3m2b4TvfIlkcXS7IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;u Mo\jQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3Mke3PVIoRjJ2NUK3O|kzRC:jPh?=
VERO MWXGeY5kfGmxbjDBd5NigQ>? NX7oenFjOjVizszN MmjWSG1UVw>? MXzEbZN1fXKkZYOgVGFTKGKnbISgd5lvfGinc3nzMEBi\m[nY4TpcochfGinIHHjeIlvKGO7dH;zb4Vt\XSxbjygZ4VtdCC|aHHw[UBidmRiY3XscEBi\Ginc3nvci=> M3TEblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{OyPFQ2Lz5{NUOzNlg1PTxxYU6=
HeLa NFrkeZZHfW6ldHnvckBCe3OjeR?= NIi2fWsyOCEQvF2= NHXiZVI1QCCq MX7S[YR2[3Srb36gc4Yh[3m2b4DsZZNucWNiZHnzeJJq[nW2aX;uJIFv\CCwdXPs[YFzKHS{YX7zcI9k[XSrb36gc4Yh|rJvY3H0[Y5qdg>? M33UPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3ME[xOFk6Lz5{NUC2NVQ6QTxxYU6=
SiHa NVqyRZA5TnWwY4Tpc44hSXO|YYm= M170T|ExKM7:TR?= NXrhNHAxPDhiaB?= MnjiVoVlfWO2aX;uJI9nKGO7dH;wcIF{dWmlIHTpd5RzcWK3dHnvckBidmRiboXjcIVieiC2cnHud4xw[2G2aX;uJI9nKM7{LXPheIVvcW5? MnjDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNkG0PVkoRjJ3ME[xOFk6RC:jPh?=
HEK293 M2LROmZ2dmO2aX;uJIF{e2G7 M1fMVmlvcGmkaYTpc44hd2ZiV17UN2Ehe2mpbnHsbY5oKGmwIFjFT|I6OyClZXzsd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmgbY4heHKnc3XuZ4Uhd2ZiZn;yd4twdGmwLDDJR|UxKD1iMD6wO|gh|ryPLh?= MmPlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NES1O|QoRjJ|OES0OVc1RC:jPh?=
DLD1 MoL0SpVv[3Srb36gZZN{[Xl? M1rrPFI1KGi{cx?= M{jtd2lvcGmkaYTpc44hd2ZidHHub5lz[XOnIHnuJIh2dWGwIFTMSFEh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIGfueEBi[3Srdnn0fUBi\nSncjCyOEBpenNiYomgWGNHNWy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygTWM2OCB;IECuO|A4KM7:TT6= NE[4dWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK5PVY5Oyd-MkWyPVk3QDN:L3G+
Sf21 NELUOHhHfW6ldHnvckBie3OjeR?= NW[5OXR5OiCqcoO= MnPxTY5pcWKrdHnvckBw\iCQLYTldo1qdmGuIFfTWE11[WepZXSgbJVu[W5iVF7LV{0zKCh6NEmgeI8hOTF4NjDy[ZNq\HWnczmg[ZhxemW|c3XkJIlvKGmwIHnud4VkfCC|ZkKxJINmdGy|IIDy[Ylv[3WkYYTl[EBnd3JiMjDodpMh\m:ubH;3[YQh[nlic4Xid5Rz[XSnIHHk[Il1cW:wIH3lZZN2emWmIHHmeIVzKDNyIH3pcpMtKEmFNUCgQUAxNjBzNzFOwG0v MmPGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzNkO1PFEoRjJ5MU[zOVgyRC:jPh?=
A673 NYrUTXhOeUiWUzDhd5NigQ>? MnfJdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN? NVfofpBWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC MX\xTHRUKGG|c3H5 Ml3xdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= MkPCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
A549 NXTueWlvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NU\sdlFHPzJiaILz NYr6PHBUT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hSTV2OTDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOTJwMzFOwG0v MmHsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl7M{SyNVkoRjJ7OUO0NlE6RC:jPh?=
Assay
Methods Test Index PMID
Western blot β-catenin / E-cadherin / N-cadherin ; β-catenin / c-Myc / cyclin D1 / E-cadherin / N-cadherin / Vimentin 31060551 28177909
Immunofluorescence β-catenin / E-cadherin ; Actin / PAR ; Hes1 / β-catenin / p-STAT3 31060551 25332845 25061499

Protocol (from reference)

Cell Research:[1]
  • 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.

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

Chemical Information

Molecular Weight 312.31
Formula

C14H11F3N2OS

CAS No. 284028-89-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CSCC2=C1N=C(NC2=O)C3=CC=C(C=C3)C(F)(F)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.

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.

Tags: buy XAV-939 | XAV-939 supplier | purchase XAV-939 | XAV-939 cost | XAV-939 manufacturer | order XAV-939 | XAV-939 distributor