U0126-EtOH

For research use only. Not for use in humans.

製品コードS1102

U0126-EtOH化学構造

分子量(MW):426.56

U0126-EtOH is a highly selective inhibitor of MEK1/2 with IC50 of 0.07 μM/0.06 μM in cell-free assays, 100-fold higher affinity for ΔN3-S218E/S222D MEK than PD98059. U0126 inhibits autophagy and mitophagy with antiviral activity.

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JPY 26400 あり
JPY 80000 あり
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バルク問合せ

文献中Selleckの製品使用例(368)

製品安全説明書

MEK阻害剤の選択性比較

生物活性

製品説明 U0126-EtOH is a highly selective inhibitor of MEK1/2 with IC50 of 0.07 μM/0.06 μM in cell-free assays, 100-fold higher affinity for ΔN3-S218E/S222D MEK than PD98059. U0126 inhibits autophagy and mitophagy with antiviral activity.
特性 A chemically synthesized and highly selective inhibitor of both MEK1 and MEK2.
ターゲット
MEK2 [1]
(Cell-free assay)
MEK1 [1]
(Cell-free assay)
0.06 μM 0.07 μM
体外試験

U0126-EtOH functionally antagonizes AP- 1 transcriptional activity and blocks the production of a variety of cytokines and metalloproteinases involved in the inflammatory response. [1] U0126-EtOH inhibits T cell proliferation in response to antigenic stimulation or cross-linked anti-CD3 plus anti-CD28 Abs without effect on IL-2-induced proliferation by down-regulating IL-2 mRNA levels. [2] A recent study shows that U0126-EtOH antagonizes resveratrol-induced apoptosis in castration-resistant human prostate cancer C4-2 cells, inhibits mitochondrial function and shifts cells to aerobic glycolysis independently of MEK. [3]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HeLa cells MU\GeY5kfGmxbjDhd5NigQ>? M1rjNWlvcGmkaYTpc44hd2ZiRVfGMZN1cW23bHH0[YQhTWytMT3seYNq\mW{YYPlJJJmeG:{dHXyJIF{e2G7IHnuJGhmVGFiY3XscJMtKEmFNUC9NE4zQSEQvF2u M3vNZ|E2OjJ3N{C2
COS-7 cells NIfBd2JHfW6ldHnvckBie3OjeR?= NX[1NppiUW6qaXLpeI9zgSClb37j[Y51emG2aX;uJIFo[Wmwc4SgRXAuOSC2cnHud4NzcXC2aX;uJIlvKEORUz23JINmdGy|78{MJGlEPTB;MTFOwG0v MX6xOVAxPjN6Nh?=
HCT116 cells Mk[4SpVv[3Srb36gZZN{[Xl? MluxRYJqdGm2eTDv[kBkd22yb4Xu[EB1dyCrbnjpZol1KGGwY3jvdoFo\SCrbnTldIVv\GWwdDDjc4xwdnliZn;ycYF1cW:wIDjzc4Z1KGGpYYKg[5Jwf3SqIHHzd4F6MSCrbjDIR3QyOTZiY3XscJMtKEmFNUC9NVkvPCEQvF2u NXfucFJiOTV{MkW3NFY>
mouse RAS-3T3 cells MojoSpVv[3Srb36gZZN{[Xl? NHTLe2EyOC12MDFOwG0> MWnJcohq[mm2aX;uJI9nKE2HSz3t[YRq[XSnZDDFVmsyNzJicHjvd5Bpd3K7bHH0bY9vKGmwIH3veZNmKFKDUz2zWFMh[2WubIOgZZQhOTBidH:gOFAhfU1iYomgSWxKW0Fw NWT2fnlsOjR3MEe4NlY>
rat PC12 cells M{n5NGZ2dmO2aX;uJIF{e2G7 MkixNVAh|ryP NIfhcmYyKGh? MofqRYN1cX[jdHnvckBw\iCQcn[yM2FTTSCrbjDyZZQhWENzMjDj[YxteyCjc4Pld5Nm\CCjczDIU{0yKHC{b4TlbY4hcW6mdXP0bY9vKGG2IEGwJJVOKGGodHXyJFUhcHK|IIDy[ZRz\WG2ZXSge4l1cCCMTlugbY5pcWKrdH;yJHNRPjByMUK1JIZweiBzIHjyJIJm\m:{ZTDjc41xd3WwZDDh[IRqfGmxbjDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? NF\EclIzOTN2NU[4OS=>

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

アッセイ
Methods Test Index PMID
Western blot
p-MEK / MEK / p-ERK / ERK; 

PubMed: 27487136     


Representative blots of MEK1/2 and ERK1/2, either total or phosphorylated, in A673 and TC71 cell lines treated with vehicle (DMSO) or 20 μM U0126. 

E-cadherin / Vimentin / Twist-2; 

PubMed: 28416770     


Western blot for E-cadherin, Vimentin, Twist-2, phoshpo-ERK1/2 and total ERK1/2 in total cell lysates of OVCAR-3-NID1-MC cells after U0126 treatment. GAPDH served as an internal control of protein loading.

27487136 28416770
Immunofluorescence
pERK / pPPARγ; 

PubMed: 27145370     


Decreased phosphorylated ERK1/2 (red) and phosphorylated PPARγ (green) with U0126 treatment in high glucose condition (30 mM). 

E-cadherin / Vimentin; 

PubMed: 28416770     


Immunofluorescent microscopic images of E-cadherin (red) and Vimentin (red) in OVCAR-3-NID1-MC cells after U0126 treatment. Nuclear was stained with 4,6-diamidino-2-phenylindole (blue) (scale bar = 20 μm).

CD40; 

PubMed: 26828592     


LB39-MEL CD70+ cells were treated with 5 μM of U0126 for 72 h then fixed and processed for immunofluorescence directed against CD70. Pictures of U0126 treated cells and control (DMSO) conditions are presented (scale bar 50 μm) 

27145370 28416770 26828592
体内試験 U0126-EtOH, as the inhibitor of intracellular Raf/MEK/ERK signaling pathway, demonstrates antiviral activity by suppressing propagation of the 2009 pandemic IV H1N1 variant and highly pathogenic avian influenza viruses (HPAIV) in vivo in the mouse lung by inhibiting. [4] U0126-EtOH shows the potential neuroprotective effect and improving spatial learning in Morris water maze (MWM) by activating peroxisome proliferator-activated receptor gamma coactivator-1a, nuclear respiratory factor 1, and mitochondrial transcription factor A in Aβ-injected rats. [5]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

- 合併

In Vitro Kinase Assays :

The amount of immunoprecipitated wild type MEK used in these assays is adjusted to give a similar amount of activity units as obtained with 10 nM recombinant MEK. Reaction velocities are measured using a 96-well nitrocellulose filter apparatus as described below. Unless otherwise noted, reactions are carried out at an enzyme concentration of 10 nM, in 20 mM Hepes, 10 mM MgCl2, 5 mM β-mercaptoethanol, 0.1 mg/mL BSA, pH 7.4, at room temperature. Reactions are initiated by the addition of [γ-33P]ATP into the premixed MEK/ERK/inhibitor reaction mixture, and an aliquot of 100 μL is taken every 6 minutes and transferred to the 96-well nitrocellulose membrane plate which has 50 mM EDTA to stop the reaction. The membrane plate is drawn and washed 4 times with buffer under vacuum. Wells are then filled with 30 μL of Microscint-20 scintillation fluid, and the radioactivity of 33P-phosphorylated ERK is counted with a Top Count scintillation counter. Velocities are obtained from the slopes of radioactivity versus time plots. Concentrations of ERK and ATP are 400 nM and 40 μM, respectively, unless otherwise indicated. For all of the in vitro enzyme assays, the percent inhibition is calculated 100 (1 −Vi/Vo) where Vi and Vo are the initial reaction velocities in the presence and absence of inhibitor, respectively. The data are then plotted as percent inhibition as a function of inhibitor concentration and fit, by nonlinear least squares regression, to the standard equation for a Langmuir isotherm to determine the IC50. As reported, enzyme concentrations are based upon molecular weights and mass of protein used in the final assay volume and not on active site titration. Thus, the actual enzyme active site concentration may differ from that reported.
細胞試験:

[2]

- 合併
  • 細胞株: A.E7 or Th17 cells
  • 濃度: 0 to 10 μM
  • 反応時間: 48 hours
  • 実験の流れ:

    A.E7 or Th17 cells are incubated with mitomycin C-treated B10.BR or BALB/c splenocytes plus varying concentrations of pigeon cytochrome c or PR8 Ag, or with 5 U/mL human rIL-2. In addition, some assays contains U0126 or an inactive analogue, U0124, to determine direct effects of MEK inhibition on T cell proliferation. Two days after culture initiation, each well is pulsed with 1 µCi of [3H]TdR and harvested the following day. The incorporation of [3H]TdR into DNA is quantitated on a Packard Matrix 96 direct beta counter without the use of liquid scintillation mixtures.


    (参考用のみ)
動物試験:

[4]

- 合併
  • 動物モデル: Female C57Bl/6 mice infected by Mouse-adapted highly pathogenic avian influenza A/FPV/Bratislava/79 (H7N7; FPV) virus and swine origin human influenza A virus (SOIV) A/Regensburg/D6/2009 (H1N1v; RB1).
  • 投薬量: ≤10 mM
  • 投与方法: Administered via aerosol.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 85 mg/mL (199.26 mM) warming
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):
10% DMSO+50% PEG 300+ddH2O
混合させたのち直ちに使用することを推奨します。
28mg/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 426.56
化学式

C18H16N6S2.C2H6O

CAS No. 1173097-76-1
Storage powder
in solvent
別名 N/A
Smiles CCO.N\C(SC1=CC=CC=C1N)=C(C#N)\C(C#N)=C(N)/SC2=CC=CC=C2N

投与溶媒組成計算器(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)
% DMSO % % Tween 80 % ddH2O
計算リセット

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 (mg) = 濃度 (mM) x 体積 (mL) 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 know whether the compound is light-sensitive?

  • 回答:

    S1102 U0126-EtOH is not stable. It should be stored as powder at -20°C, and prepared the solution just before use.

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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