U0126-EtOH

製品コードS1102 バッチS110208

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C18H16N6S2.C2H6O
分子量 426.56 CAS No. 1173097-76-1
Solubility (25°C)* 体外 DMSO 85 mg/mL (199.26 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 4.250mg/ml (9.96mM) Taking the 1 mL working solution as an example, add 50 μL of 85 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

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.
in vitro

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] This compound 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 this chemical 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]
in vivo

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] This compound 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]
特徴 A chemically synthesized and highly selective inhibitor of both MEK1 and MEK2.

プロトコル(参考用のみ)

キナーゼアッセイ 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/this compound 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 this chemical, respectively. The data are then plotted as percent inhibition as a function of this compound 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.
細胞アッセイ 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 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-EtOH 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.
動物実験 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

  • https://pubmed.ncbi.nlm.nih.gov/9873633/
  • https://pubmed.ncbi.nlm.nih.gov/9574517/
  • https://pubmed.ncbi.nlm.nih.gov/22108021/
  • https://pubmed.ncbi.nlm.nih.gov/21854809/
  • https://pubmed.ncbi.nlm.nih.gov/22510382/
  • https://pubmed.ncbi.nlm.nih.gov/9660836/

カスタマーフィードバック

Data from [Proc Natl Acad Sci U S A, 2014, 111(15):E1528-37]

Data from [Biochim Biophys Acta, 2013, 1832(12):1998-2008]

Data from [Biochim Biophys Acta, 2013, 1832(12):1998-2008]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

GRB2 regulation of essential signaling pathways in the endometrium is critical for implantation and decidualization [ Nat Commun, 2025, 16(1):2192] PubMed: 40038241
Nucleus-translocated glucokinase functions as a protein kinase to phosphorylate TAZ and promote tumour growth [ Nat Commun, 2025, 16(1):7156] PubMed: 40759645
Enhancing Tendon Regeneration: Investigating the Impact of Topography on the Secretome of Adipose-Derived Stem Cells [ Adv Sci (Weinh), 2025, 12(18):e2417447] PubMed: 40091553
Quercetin ameliorates oxidative stress in BMP15-deficient oocytes by regulating the ERK1/2-GSK3β-CypD pathway [ Redox Biol, 2025, 87:103886] PubMed: 41086612
PlexinD1 is a driver and a therapeutic target in advanced prostate cancer [ EMBO Mol Med, 2025, 17(2):336-364] PubMed: 39748059
Active R-RAS2/TC21 prevents cell cycle arrest and morphological alterations in mouse embryonic fibroblasts lacking RAS proteins [ Oncogene, 2025, 10.1038/s41388-025-03367-3] PubMed: 40164870
TLR4 endocytosis and endosomal TLR4 signaling are distinct and independent outcomes of TLR4 activation [ EMBO Rep, 2025, 10.1038/s44319-025-00444-2] PubMed: 40204912
ERK1-mediated GLYCTK2 phosphorylation promotes fructolysis to sustain glioblastoma survival under glucose deprivation [ Cell Death Discov, 2025, 11(1):266] PubMed: 40467571
Nbeal2 Inactivation Triggers Abl1 Stabilisation and Dysregulated Subcellular Localisation of the Multi-Drug-Resistant Protein MDR1 (ABCB1) in Mast Cells [ Immunology, 2025, NONE] PubMed: 41111259
Erk1/2 Orchestrates SSPH I-Induced Oxidative Stress, Mitochondrial Dysfunction and Ferroptosis in Hepatocellular Carcinoma [ J Cell Mol Med, 2025, 29(10):e70609] PubMed: 40394754

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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