U0126-EtOH

Catalog No.S1102

For research use only.

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.

U0126-EtOH Chemical Structure

CAS No. 1173097-76-1

Selleck's U0126-EtOH has been cited by 662 publications

Purity & Quality Control

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Biological Activity

Description 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.
Features A chemically synthesized and highly selective inhibitor of both MEK1 and MEK2.
Targets
MEK2 [1]
(Cell-free assay)
MEK1 [1]
(Cell-free assay)
0.06 μM 0.07 μM
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] 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
rat PC12 cells Mmi0SpVv[3Srb36gZZN{[Xl? NVrPSnJxOTBizszN MWmxJIg> M13nO2FkfGm4YYTpc44hd2ZiToLmNk9CWkViaX6gdoF1KFCFMUKgZ4VtdHNiYYPz[ZN{\WRiYYOgTG8uOSCycn;0[YlvKGmwZIXjeIlwdiCjdDCxNEB2VSCjZoTldkA2KGi{czDwdoV1emWjdHXkJJdqfGhiSl7LJIlvcGmkaYTvdkBUWDZyMEGyOUBnd3JiMTDodkBj\W[xcnWgZ49ueG:3bnSgZYRlcXSrb36gZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| NV3DO2s3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzOFU3QDVpPkKxN|Q2Pjh3PD;hQi=>
mouse RAS-3T3 cells MWfGeY5kfGmxbjDhd5NigQ>? NHPafZEyOC12MDFOwG0> M1exVmlvcGmkaYTpc44hd2ZiTVXLMY1m\GmjdHXkJGVTUzFxMjDwbI9{eGixconsZZRqd25iaX6gcY92e2ViUlHTMVNVOyClZXzsd{BifCBzMDD0c{A1OCC3TTDifUBGVEmVQT6= NYLnNIlpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1NFc5OjZpPkK0OVA4QDJ4PD;hQi=>
HCT116 cells NEnZOmJHfW6ldHnvckBie3OjeR?= MWHBZoltcXS7IH;mJINwdXCxdX7kJJRwKGmwaHnibZQh[W6laH;yZYdmKGmwZHXw[Y5l\W62IHPvcI9vgSCob4LtZZRqd25iKIPv[pQh[WejcjDndo94fGhiYYPzZZkqKGmwIFjDWFEyPiClZXzsd{whUUN3ME2xPU41KM7:TT6= NWrnVIJQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUWyNlU4ODZpPkG1NlI2PzB4PD;hQi=>
COS-7 cells M1TJZ2Z2dmO2aX;uJIF{e2G7 MVXJcohq[mm2b4L5JINwdmOnboTyZZRqd25iYXfhbY5{fCCDUD2xJJRz[W6|Y4LpdJRqd25iaX6gR29UNTdiY3XscJPwxIxiSVO1NF0yKM7:TT6= NX7HSIt{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUWwNFY{QDZpPkG1NFA3Ozh4PD;hQi=>
HeLa cells NYHB[XN7TnWwY4Tpc44h[XO|YYm= NYfFXJR1UW6qaXLpeIlwdiCxZjDFS2Yue3SrbYXsZZRm\CCHbHuxMYx2[2moZYLhd4UhemWyb4L0[ZIh[XO|YYmgbY4hUGWOYTDj[YxteyxiSVO1NF0xNjJ7IN88UU4> M3fzcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3MkK1O|A3Lz5zNUKyOVcxPjxxYU6=
Assay
Methods Test Index PMID
Western blot p-MEK / MEK / p-ERK / ERK ; E-cadherin / Vimentin / Twist-2 27487136 28416770
Immunofluorescence pERK / pPPARγ ; E-cadherin / Vimentin ; CD40 27145370 28416770 26828592
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] 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]

Protocol (from reference)

Kinase Assay:

[1]

  • 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.

Cell Research:

[2]

  • Cell lines: A.E7 or Th17 cells
  • Concentrations: 0 to 10 μM
  • Incubation Time: 48 hours
  • Method:

    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.

Animal Research:

[4]

  • Animal Models: 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).
  • Dosages: ≤10 mM
  • Administration: Administered via aerosol.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5%DMSO+40%PEG300+5%Tween 80+50%H2O
For best results, use promptly after mixing.

4.25mg/mL

Chemical Information

Molecular Weight 426.56
Formula

C18H16N6S2.C2H6O

CAS No. 1173097-76-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCO.C1=CC=C(C(=C1)N)SC(=C(C#N)C(=C(N)SC2=CC=CC=C2N)C#N)N

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
I want to know whether the compound is light-sensitive?

Answer:
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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