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Cat. No. M1977
U0126-EtOH Structure

CAS# 109511-58-2

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5mg USD 30  USD30 In stock
10mg USD 45  USD45 In stock
25mg USD 80  USD80 In stock
50mg USD 130  USD130 In stock
100mg USD 160  USD160 In stock
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Biological Activity

U0126-EtOH is a highly selective inhibitor of both MEK1 and MEK2, a type of MAPK/ERK kinase. U0126 inhibited anchorage-independent growth of Ki-ras-transformed rat fibroblasts by simultaneously blocking both extracellular signal-regulated kinase (ERK) and mammalian target of rapamycin (mTOR)-p70(S6K) pathways. U0126 inhibits MEK-1 and MEK-2 with little or no effect on the activities of PKC, Abl, Raf, MEKK, ERK, JNK, MKK-3, MKK-4/SEK, MKK-6, Cdk2 or Cdk4. U0126 selectively repressed anchorage-independent growth of MDA-MB231 and HBC4 cells, two lines with constitutively activated ERK. In addition, i.v. administration of U0126 (100-200 mg/kg), a specific inhibitor of MEK (MAPK/ERK kinase), protects the hippocampus against forebrain ischemia. Moreover, treatment with U0126 at 3 h after ischemia significantly reduces infarct volume after transient (3 h) focal cerebral ischemia in mice. 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.

Product Citations
Customer Product Validations & Biological Datas
Source J Immunol (2018 Oct). Figure 3. U0126 (AbMole BioScience)
Method Western blots
Cell Lines DCs
Concentrations 10 μM
Incubation Time 30 min
Results The addition of NF-kB- and JNK-specific inhibitors signifi-cantly attenuated the KRS-induced IL-12 production from DCs, whereas p38 kinase and ERK inhibitors only slightly affected the IL-12 production from KRS-treated DCs.
Source BMC Genomics (2017). Additional file 7. U0126 (Abmole Bioscience, USA)
Method qRT-PCR
Cell Lines pupa abdomen
Incubation Time 48 h
Results We performed injection experiments involving several inhibitors of the insulin signaling pathway. It was observed that the development of follicles was clearly delayed and the follicles showed abnormalities (Additional file 7), and the expressions of marker genes, like Cyp18a1 and early chorion gene, were up-regulated at choriogenic stages.
Source International Immunopharmacology(2016).Figure 4. U0126 (AbMole BioScience, Houston, TX)
Method CD4+ T cell isolation and T cell polarization in vitro
Cell Lines CD4+ T cells
Concentrations 0.5–2.0 μM
Incubation Time
Results When CD4+ T cells were treated with costunolide, U0126, or SB203580, the expression of CD69 upon TCR stimulation was significantly down-regulated (Fig. 4B). Th1 and Th2 cell generation was suppressed when ERK activation was inhibited by U0126 in a similar fashion to that of costunolide, albeit the development of Th17 cells was unchanged in the presence of U0126 (Fig. 4C).
Protocol (for reference only)
Cell Experiment
Cell lines EHMES-10 cells and MSTO211H cells
Preparation method Cell proliferation assay. The cell proliferation assay reagent WST-1 (4-[3-(4-lodophenyl)-2-(4-nitrophenyl)-2H-5-tetrazolio]- 1,3-benzene disulfonate) (Roche Diagnostics GmbH, Mannheim, Germany) was used to assess the effect of U0126 or LY294002 on cell growth. MPM cells (1x104 cells/well) were plated in 96-well plates (Nunc, Roskilde, Denmark) and were exposed to various concentrations of test agents dissolved in DMSO. Controls received DMSO vehicle at a concentration equal to that of drug treated cells. After drug treatment for 72 h, 10 µl of WST-1 reagent were added to each well. Absorbance was measured at 450 nm with a reference wavelength at 690 nm by an E max precision microplate reader (Molecular Devices, Tokyo, Japan).
Concentrations 0~200µM
Incubation time 72 h
Animal Experiment
Animal models Orthotopic implantation model
Formulation DMSO + PBS
Dosages 20, 30 and 40 mg/kg twice a week
Administration intraperitoneally
Chemical Information
Molecular Weight 426.56
Formula C18H16N6S2.C2H6O
CAS Number 1173097-76-1
Solubility (25°C) DMSO ≥ 50 mg/mL (warmed)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Priscila B Rosa, et al. Purinergic Signal. The antidepressant-like effect of guanosine is dependent on GSK-3β inhibition and activation of MAPK/ERK and Nrf2/heme oxygenase-1 signaling pathways

[2] Satoshi Deyama, et al. Int J Neuropsychopharmacol. Resolvin D1 and D2 Reverse Lipopolysaccharide-Induced Depression-Like Behaviors Through the mTORC1 Signaling Pathway

[3] Ana Lucia Bertarello Z, et al. Pharmacol Biochem Behav. Involvement of PKA, CaMKII, PKC, MAPK/ERK and PI3K in the acute antidepressant-like effect of ferulic acid in the tail suspension test

[4] Namura S, et al. Proc Natl Acad Sci U S A. Intravenous administration of MEK inhibitor U0126 affords brain protection against forebrain ischemia and focal cerebral ischemia.

[5] Duncia JV, et al. Bioorg Med Chem Lett. MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products.

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Keywords: U0126-EtOH, CAS# 109511-58-2 supplier, MEK, inhibitors, activators

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