XAV-939

製品コードS1180 別名:NVP-XAV939

XAV-939化学構造

分子量(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.

サイズ 価格(税別)  
JPY 15106.00
JPY 11620.00
JPY 28220.00
JPY 44820.00
JPY 127820.00

カスタマーフィードバック(7)

  • 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, 2017, 400:194-202. 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.

製品安全説明書

Wnt/beta-catenin阻害剤の選択性比較

生物活性

製品説明 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.
ターゲット
TNKS2 [1]
(Cell-free assay)
TNKS1 [1]
(Cell-free assay)
4 nM 11 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf-21 MoX5T4lv[XOnIFHzd4F6 M2\OW|E5Njd3IN88US=> NV7ObJNUPjBibXnu NUj1dFVyTE2VTx?= MlXsTY5pcWKrdHnvckBw\iCQLYTldo1qdmGuIFfTWE11[WepZXSgWG5MWzJiZYjwdoV{e2WmIIfpeIghUUN3MDDv[kAxNjByNUOg{txO MXuyN|g4QTR|MR?=
HEK293T M{LrOWZ2dmO2aX;uJGF{e2G7 MmW4SG1UVw>? NITtZZBKdmirYnn0bY9vKG:oIGfueEB{cWewYXzpcoch[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBnd3K|a3;sbY4ucW6mdXPl[EBkSU2SIILld5BwdnOnIHXs[Y1mdnRiYXP0bZZifGmxbjD3bZRpKEmFNUCgc4YhOC5yN{ig{txO NIrMbXYzOzh5OUSzNS=>
HEK293T NUfO[YJ1TnWwY4Tpc44hSXO|YYm= MVSxNEDPxE1? NELaSXBFVVOR NVHy[ZFJUW6qaXLpeIlwdiCxZjDi[ZRiNWOjc3Xpck1l\XCnbnTlcpQh[2Gwb37pZ4FtKFewdEOgdIF1cHejeTD3bZRpKEmFNUCgc4YhOC5yNUGg{txO MoPPNlIyQTF3NUe=
HEK293T Mom2SpVv[3Srb36gRZN{[Xl? M4na[FI1KGh? M1fsWWROW09? NV\BdnpkUW6qaXLpeIlwdiCxZjDtc5V{\SCZboSzRUB{cWewYXzpcochf2m2aDDJR|UxKG:oIECuNFc5KM7:TR?= NF;OfZQzOjJ4MEKwNy=>
SW480 MXvGeY5kfGmxbjDBd5NigQ>? M{j6O|ExKM7:TR?= NF;sOmUzPCCq NEGyXFFFVVOR MlfFV5Ri[mmuaYrheIlwdiCxZjDBfIlvOiC5aYToJGVEPTBib3[gNE4{PzFizszN NH:0S3YzOjJ4MEKwNy=>
HEK293T NGjEb3FHfW6ldHnvckBCe3OjeR?= MVK1NEDPxE1? NXvCTYhETE2VTx?= MXjIZZMhdm9iRX\m[YN1KG:wIH\vdpNsd2yrbj3pcoR2[2WmIHPBUXAhe2mpbnHsbY5oKGmwIHj1cYFvKEiHS{K5N3Qh[2WubIOgZ49mgHC{ZYPzbY5oKEOURR?= MoSyNlIzPjB{MEO=
IEC-6 M4X5e2Z2dmO2aX;uJGF{e2G7 M{j2XVYhcA>? MnHWRY51[WexbnnzeEBi[3Srdnn0fUBifCCEZYThMYNifGWwaX6vWGNHKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhX262LUPhMYlv\HWlZXSgZZhqdjJiZYjwdoV{e2mxbjD3bZRpKEmFNUCgc4YhOC54NDFOwG0> M3i4clI1ODZyNEi5
IEC-6 NFzKW5FHfW6ldHnvckBCe3OjeR?= M{DtSlYhcA>? NHvYV41CdnSjZ3;ubZN1KGGldHn2bZR6KGG2IFLleIEu[2G2ZX7pck9VS0ZiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCZboStN4EucW6mdXPl[EBt\3J3IHX4dJJme3Orb36ge4l1cCCLQ{WwJI9nKDJwOTFOwG0> NYLWXIJKOjRyNkC0PFk>
DLD1 NG\4WoVHfW6ldHnvckBCe3OjeR?= NEHEb4EzOCEQvF2= M{TCbFI1KGh? M{nVW2ROW09? MmPlTY5pcWKrdHnvckBw\iC2YX7rfZJie2ViYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCWQ1[t[IVx\W6mZX70JJRz[W6|Y4LpdJRqd26jbDDhZ5Rqfmm2eR?= MlX1NlQ2Ojd5OUK=
DLD1 M4jwT2N6fG:2b4jpZ{BCe3OjeR?= MVmyNEDPxE1? MnXqNVAh\A>? NVrGR5FrTE2VTx?= MkXtR5l1d3SxeHnjbZR6KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:w MYGyOFUzPzd7Mh?=
VERO MV\GeY5kfGmxbjDBd5NigQ>? NXrqWJlrOjVizszN MYrEUXNQ MV;EbZN1fXKkZYOgVGFTKGKnbISgd5lvfGinc3nzMEBi\m[nY4TpcochfGinIHHjeIlvKGO7dH;zb4Vt\XSxbjygZ4VtdCC|aHHw[UBidmRiY3XscEBi\Ginc3nvci=> NVjHWGd7OjV|M{K4OFU>
HeLa MWTGeY5kfGmxbjDBd5NigQ>? MU[xNEDPxE1? MWW0PEBp NVXBOI84WmWmdXP0bY9vKG:oIHP5eI9xdGG|bXnjJIRqe3S{aXL1eIlwdiCjbnSgcpVkdGWjcjD0doFve2yxY3H0bY9vKG:oIN8yMYNifGWwaX6= MofhNlUxPjF2OUm=
SiHa MnjOSpVv[3Srb36gRZN{[Xl? NYPrcnQzOTBizszN NYnkV2kyPDhiaB?= NHzO[oFT\WS3Y4Tpc44hd2ZiY4n0c5Bt[XOvaXOg[Il{fHKrYoX0bY9vKGGwZDDueYNt\WG{IITyZY5{dG:lYYTpc44hd2ZizsKtZ4F1\W6rbh?= MnHNNlUxPjF2OUm=

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

お薦めの試験操作(参考用のみ)

細胞試験: [1]
+ 展開
  • 細胞株: WTK1 lymphoblasts
  • 濃度: 1.0 μM
  • 反応時間: 8 hours
  • 実験の流れ: 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.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 12 mg/mL (38.42 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
4% DMSO+corn oil
混合させたのち直ちに使用することを推奨します。
1mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 312.31
化学式

C14H11F3N2OS

CAS No. 284028-89-3
保管
in solvent
別名 NVP-XAV939

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問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.

  • 回答:

    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シグナル伝達経路

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID