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はtankyrase1/2を抑制することを通じて、Wnt/β-cateninが媒介した転写を選択制的に抑制して、無細胞試験でIC50値が11 nM/4 nMになりますが、アキシンレベル(axin level)を調節して、 CRE、NF-κBとTGF-βに作用を表しません。

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JPY 13102.90 あり
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JPY 24477.96 あり
JPY 38876.76 あり
JPY 110870.76 あり

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, 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.

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はtankyrase1/2を抑制することを通じて、Wnt/β-cateninが媒介した転写を選択制的に抑制して、無細胞試験でIC50値が11 nM/4 nMになりますが、アキシンレベル(axin level)を調節して、 CRE、NF-κBとTGF-βに作用を表しません。
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 M4PWW2tqdmG|ZTDBd5NigQ>? MmTSNVgvPzVizszN Mkf4OlAhdWmw M1TwTmROW09? NEfkW2pKdmirYnn0bY9vKG:oIF6teIVzdWmwYXygS3NVNXSjZ3fl[EBVVkuVMjDlfJBz\XO|ZXSge4l1cCCLQ{WwJI9nKDBwMEC1N{DPxE1? NUTLWmd3OjN6N{m0N|E>
HEK293T M{TwdmZ2dmO2aX;uJGF{e2G7 NUXJcWIxTE2VTx?= NIKxcJVKdmirYnn0bY9vKG:oIGfueEB{cWewYXzpcoch[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBnd3K|a3;sbY4ucW6mdXPl[EBkSU2SIILld5BwdnOnIHXs[Y1mdnRiYXP0bZZifGmxbjD3bZRpKEmFNUCgc4YhOC5yN{ig{txO MmP1NlM5Pzl2M{G=
HEK293T M1XJUmZ2dmO2aX;uJGF{e2G7 NIToWHcyOCEQvF2= NHj5fZFFVVOR MX;Jcohq[mm2aX;uJI9nKGKndHGtZ4F{\WmwLXTldIVv\GWwdDDjZY5wdmmlYXygW451OyCyYYToe4F6KHerdHigTWM2OCCxZjCwMlA2OSEQvF2= M{T2RlIzOTlzNUW3
HEK293T NV\4WnB7TnWwY4Tpc44hSXO|YYm= MV[yOEBp Mn[xSG1UVw>? NUfqS5k3UW6qaXLpeIlwdiCxZjDtc5V{\SCZboSzRUB{cWewYXzpcochf2m2aDDJR|UxKG:oIECuNFc5KM7:TR?= MYiyNlI3ODJyMx?=
SW480 NFLRcoVHfW6ldHnvckBCe3OjeR?= MV2xNEDPxE1? M{XPbVI1KGh? MmrBSG1UVw>? M2PtcXN1[WKrbHn6ZZRqd25ib3[gRZhqdjJid3n0bEBGSzVyIH;mJFAvOzdzIN88US=> M3rOVlIzOjZyMkCz
HEK293T M1[xd2Z2dmO2aX;uJGF{e2G7 Mmm2OVAh|ryP NEL6Wm5FVVOR NXrBR4hTUGG|IH7vJGVn\mWldDDvckBnd3K|a3;sbY4ucW6mdXPl[EBkSU2SIIPp[45idGmwZzDpckBpfW2jbjDISWszQTOWIHPlcIx{KGOxZYjwdoV{e2mwZzDDVmU> MnjNNlIzPjB{MEO=
IEC-6 NHi0O5JHfW6ldHnvckBCe3OjeR?= NXXJcm1xPiCq M4mxNWFvfGGpb37pd5Qh[WO2aY\peJkh[XRiQnX0ZU1k[XSnbnnuM3RETiCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKFewdD2zZU1qdmS3Y3XkJIF5cW5{IHX4dJJme3Orb36ge4l1cCCLQ{WwJI9nKDBwNkSg{txO NVvhc|BtOjRyNkC0PFk>
IEC-6 M3f2VmZ2dmO2aX;uJGF{e2G7 M{Xs[|YhcA>? NGXGNYdCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IFLleIEu[2G2ZX7pck9VS0ZiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCZboStN4EucW6mdXPl[EBt\3J3IHX4dJJme3Orb36ge4l1cCCLQ{WwJI9nKDJwOTFOwG0> NYTqbJNmOjRyNkC0PFk>
DLD1 NFjGVJBHfW6ldHnvckBCe3OjeR?= NFrqemQzOCEQvF2= MmTzNlQhcA>? NVnON3R7TE2VTx?= MU\Jcohq[mm2aX;uJI9nKHSjbnv5doF{\SCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKFSFRj3k[ZBmdmSnboSgeJJidnOlcnnweIlwdmGuIHHjeIl3cXS7 M3HHWFI1PTJ5N{my
DLD1 NU\vcmJ3S3m2b4TvfIlkKEG|c3H5 NYjYT2tGOjBizszN NFi1V4UyOCCm MmXoSG1UVw>? MX3DfZRwfG:6aXPpeJkh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25? MknlNlQ2Ojd5OUK=
VERO MoOySpVv[3Srb36gRZN{[Xl? MoTNNlUh|ryP M{Pa[mROW09? MYDEbZN1fXKkZYOgVGFTKGKnbISgd5lvfGinc3nzMEBi\m[nY4TpcochfGinIHHjeIlvKGO7dH;zb4Vt\XSxbjygZ4VtdCC|aHHw[UBidmRiY3XscEBi\Ginc3nvci=> MkHVNlU{OzJ6NEW=
HeLa NFHFPXBHfW6ldHnvckBCe3OjeR?= NVLSUFJ6OTBizszN MYK0PEBp MV\S[YR2[3Srb36gc4Yh[3m2b4DsZZNucWNiZHnzeJJq[nW2aX;uJIFv\CCwdXPs[YFzKHS{YX7zcI9k[XSrb36gc4Yh|rJvY3H0[Y5qdg>? NGPXfpQzPTB4MUS5PS=>
SiHa M{\Td2Z2dmO2aX;uJGF{e2G7 NEji[moyOCEQvF2= NFnwVFQ1QCCq MnTxVoVlfWO2aX;uJI9nKGO7dH;wcIF{dWmlIHTpd5RzcWK3dHnvckBidmRiboXjcIVieiC2cnHud4xw[2G2aX;uJI9nKM7{LXPheIVvcW5? M1[0bFI2ODZzNEm5

多くの細胞株試験データを見る場合、クリックしてください

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 順序で溶剤を入れること:
30% PEG 400+0.5% Tween 80+5% Propylene glycol
30mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)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

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    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

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、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 ( 輸入 輸出 )

  • 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

マス 濃度 ボリューム 分子量

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

よくある質問(FAQ)

  • 問題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信号経路図

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Tags: XAV-939を買う | XAV-939 ic50 | XAV-939供給者 | XAV-939を購入する | XAV-939費用 | XAV-939生産者 | オーダーXAV-939 | XAV-939化学構造 | XAV-939分子量 | XAV-939代理店
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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