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U0126

Cat. No. M1977
U0126 Structure
Size Price Availability Quantity
10mg USD 65 In stock
50mg USD 160 In stock
100mg USD 240 In stock
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Quality Control
Biological Activity

U0126 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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 380.48
Formula C18H16N6S2
CAS Number 109511-58-2
Purity 99.40%
Solubility DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
Source BMC Genomics (2017). Additional file 7. U0126 (Abmole Bioscience, USA)
Method qRT-PCR
Cell Lines pupa abdomen
Concentrations
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.
Rating
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).
Rating
Product Citations
References

Intravenous administration of MEK inhibitor U0126 affords brain protection against forebrain ischemia and focal cerebral ischemia.
Namura S, et al. Proc Natl Acad Sci U S A. 2001 Sep 25;98(20):11569-74. PMID: 11504919.

MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products.
Duncia JV, et al. Bioorg Med Chem Lett. 1998 Oct 20;8(20):2839-44. PMID: 9873633.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: U0126 supplier, MEK, inhibitors

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