U0126-EtOH

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.

サイズ 価格(税別)  
JPY 24402.00
JPY 78020.00

文献中の使用例(62)

カスタマーフィードバック(13)

  •  

    Melanoma cell viability and in vivo growth by cyclindependent kinase 2/4 inhibition. Western blot analysis for c-Jun, phosphorylated-ERK1/2 (Thr202/Tyr204) (p-ERK1/2), and total ERK1/2 protein levels was done for human melanoma cell lines treated with the BRAFV600E inhibitor GDC-0879 (1 μM), or MEK inhibitors CI-1040 (1 μM), U0126 (1 μM), and PD98059 (10 μM) for 18 hours.

    J Natl Cancer Inst 2012 104(21), 1673-9. U0126-EtOH purchased from Selleck.

    Cells were stimulated with TPA (10 nM) for 15 min in the presence of the indicated concentrations of U0126. Samples were collected and analyzed by Western blot to detect phosphorylated p42/p44 MAPK.

    Proc Natl Acad Sci U S A 2014 111(15):E1528-37. U0126-EtOH purchased from Selleck.

  • Successful test of decision tree model prediction that reducing ERK signal on Cn/tEGF substrates will enhance MSC migration persistence and mean free path. (A) mean free path, (B) persistence time, and (C) speed under partial and total ERK inhibition with MEK inhibitor U0126

    Biomaterials 2011 32, 7524-7531. U0126-EtOH purchased from Selleck.

    Inhibition of the ERK1/2 pathway prevents FLIPL downregulation and sensitivity to TRAIL induced by EGF. MCF10A cells were preincubated in the absence of EGF for 48 h before re-addition of EGF ( -/+ ) and incubated in the presence or absence of ( a) the PI3K inhibitor LY294002 (LY, 10 μM), or (b) the MEK1 inhibitor U0126 (10 μM), for 15 h. Other cultures were incubated in parallel with (+/+ ) or without ( -/- ) EGF for the entire experimental period (preincubation/incubation). FLIPL , p-AKT, AKT, p-ERK1/2, ERK1/2 and BimEL levels were assessed by western blotting. GAPDH and tubulin levels were used as protein loading controls. FLIPL mRNA levels were measured by quantitative PCR (b , lower panel). Results are representative of two independent experiments. (c ) Cells were preincubated/incubated as in (b) and then TRAIL (500 ng/ml) was added to some cultures for 6 h. Apoptosis was determined as described in Materials and Methods. Error bars represent S.D. from three independent experiments.

    Cell Death Differ 2012 19, 1908-16. U0126-EtOH purchased from Selleck.

  • UACC62 cells were treated for 6 hours as indicated, followed by assessment of phospho-p90RSK1 and p90RSK1 levels by western blotting.

    J Invest Dermatol 2012 132, 2780-90. U0126-EtOH purchased from Selleck.

    SB431542(10 μM) and U0126EtOH (8 μM), which can inhibit of EMT were used to treat HCT-116 and HCT-8 in these experiments. (A) Protein expression levels of EMT markers E-cd, Claudin-4 and Vim in CRC cells. *P < 0.05.

    Sci Rep, 2016, 6:37534. U0126-EtOH purchased from Selleck.

  • ERK activation is increased in Il6ra2/2 mice compared with WT mice. A, Total and phosphorylated (p) Stat3 and ERK were assessed in small punch biopsy wounds collected after 30 min (Stat3) or 1 d (ERK) by Western blotting. Densitometry results for the blots are provided to the right. pp , 0.05. B, Total and p-ERKs were assessed in small wounds generated in WTand Il6ra2/2 mice treated topically with vehicle (DMSO) or with the MEK inhibitor U0126.Wounds were harvested after 1 d, and western blotting was performed on lysates. C, Wound contraction was assessed macroscopically in large wounds of WT (left panel) and Il6ra2/2 mice treated daily with vehicle (DMSO) or U0126. pp , 0.05.

    J Immunol 2010 184, 7219-7228. U0126-EtOH purchased from Selleck.

    Dose response curves and cytotoxic CI plots for A549 in 72 h combined treatment of gemcitacine, AG1478 and U0126 are shown in (A) and (B), respectively. These are also shown for H322 in (C) and (D). Gemcitabine concentration was set constant at 10 nM for A549 and 500 nM for H322. U0126 concentration was 2.5 μM and AG1478.

    Lung Cancer 2011 73, 274-82. U0126-EtOH purchased from Selleck.

  • Protein levels of p-MEK1/2, p-ERK1/2 and Rad51. The cells were treated with the indicated agents for 24 h (T0.5 represents 0.5 mg/mL of TGS; M0.5, M1, M2 represent 0.5, 1 and 2 μg/mL of MMC, respectively; MT 0.5 represents 0.25 mg/mL TGS+0.5 μg/mL MMC; MT 1 represents 0.5 mg/mL TGS+1 μg/mL MMC; MT2 represents 1 mg/mL TGS+2 μg/mL MMC), U0126 (10 μmol/L) was used as MEK1/2 inhibitor. GAPDH served as the loading control.

    Acta Pharmacol Sin, 2018, 39(3):449-458. U0126-EtOH purchased from Selleck.

    Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of U0126 for 24 hours.

    2010 Dr. Zhang of Tianjin Medical University. U0126-EtOH purchased from Selleck.

  • Some of the mice received intra-peritoneal administration of U0126 (10 mg/kg BW) or vehicle beginning at 24 h after I/R or sham until 24 h prior to harvest daily. Antibodies used was: Na,K-ATPase.

    Biochim Biophys Acta 2013 1832(12):1998-2008. U0126-EtOH purchased from Selleck.

    Some of the mice received intra-peritoneal administration of U0126 (10 mg/kg BW) or vehicle beginning at 24 h after I/R or sham until 24 h prior to harvest daily. kidneys were snap-frozen in liquid nitrogen and perfusion-fixed with 30 mL of phosphate buffered saline (PBS) for 2 min and then PLP (4% paraformaldehyde, 75 mM l-lysine, 10 mM sodium periodate) solution, respectively.

    Biochim Biophys Acta 2013 1832(12):1998-2008. U0126-EtOH purchased from Selleck.

  • U0126-EtOH purchased from Selleck.

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.
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 MXrGeY5kfGmxbjDhd5NigQ>? NUP3[I44UW6qaXLpeIlwdiCxZjDFS2Yue3SrbYXsZZRm\CCHbHuxMYx2[2moZYLhd4UhemWyb4L0[ZIh[XO|YYmgbY4hUGWOYTDj[YxteyxiSVO1NF0xNjJ7IN88UU4> NGj6VY8yPTJ{NUewOi=>
COS-7 cells Mn3ESpVv[3Srb36gZZN{[Xl? MnXsTY5pcWKrdH;yfUBkd26lZX70doF1cW:wIHHnZYlve3RiQWCtNUB1emGwc3PybZB1cW:wIHnuJGNQWy15IHPlcIx{97zOIFnDOVA:OSEQvF2u Mne5NVUxODZ|OE[=
HCT116 cells NIqzV2RHfW6ldHnvckBie3OjeR?= M2X3R2FjcWyrdImgc4Yh[2:vcH;1coQhfG9iaX7obYJqfCCjbnPoc5Ji\2ViaX7k[ZBmdmSnboSgZ49td267IH\vdo1ifGmxbjCod49nfCCjZ3HyJIdzd3e2aDDhd5NigSliaX6gTGNVOTF4IHPlcIx{NCCLQ{WwQVE6NjRizszNMi=> MYexOVIzPTdyNh?=
mouse RAS-3T3 cells NWX2cmgzTnWwY4Tpc44h[XO|YYm= MmnJNVAuPDBizszN NFq3VopKdmirYnn0bY9vKG:oIF3FT{1u\WSrYYTl[EBGWktzL{KgdIhwe3Cqb4L5cIF1cW:wIHnuJI1wfXOnIGLBV{0{XDNiY3XscJMh[XRiMUCgeI8hPDBidV2gZpkhTUyLU1Gu NFW5WpQzPDVyN{iyOi=>
rat PC12 cells MnviSpVv[3Srb36gZZN{[Xl? M1POeFExKM7:TR?= M4TVbVEhcA>? M4ftR2FkfGm4YYTpc44hd2ZiToLmNk9CWkViaX6gdoF1KFCFMUKgZ4VtdHNiYYPz[ZN{\WRiYYOgTG8uOSCycn;0[YlvKGmwZIXjeIlwdiCjdDCxNEB2VSCjZoTldkA2KGi{czDwdoV1emWjdHXkJJdqfGhiSl7LJIlvcGmkaYTvdkBUWDZyMEGyOUBnd3JiMTDodkBj\W[xcnWgZ49ueG:3bnSgZYRlcXSrb36gZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| M1v0RVIyOzR3Nki1

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

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]

+ 展開

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]

+ 展開
  • 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]

+ 展開
  • 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).
  • 製剤: U0126-EtOH is dissolved in 10% DMSO, 30% of Cremophor EL and 60% PBS.
  • 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:
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
保管
in solvent
別名 N/A

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