1. MAPK/ERK Pathway
    Autophagy
  2. MEK
    Autophagy

U0126 (Synonyms: U0126-EtOH)

Cat. No.: HY-12031 Purity: 98.03%
Data Sheet SDS Handling Instructions

U0126 is a non-ATP competitive MEK inhibitor, with IC50 of 70 nM and 60 nM for MEK1 and MEK2, respectively.

For research use only. We do not sell to patients.
U0126 Chemical Structure

U0126 Chemical Structure

CAS No. : 1173097-76-1

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10 mM * 1 mL in DMSO $55 In-stock
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Customer Review

    U0126 purchased from MCE. Usage Cited in: ACS Chem Neurosci. 2015 Jan 21;6(1):130-7.

    U0126 protects PC12 cells against H2O2-induced cell death. Western blot of ERK phosphorylation demonstrates that the MEK inhibitors U0126, Trametinib and Pimasertib are effective in blocking ERK phosphorylation under complete media, while U0124 results in slight ERK inhibition compared to DMSO control. Serum starvation results in lack of ERK phosphorylation in all conditions.

    U0126 purchased from MCE. Usage Cited in: Cell Signal. 2017 Jan 16;32:48-58. 

    Western blotting showing the hepaCAMexpression and the phosphorylation level of STAT3, ERK and AKT in cells treated with IL-6 (20 ng/mL) for 24 h with or without the pretreatment of two respective inhibitors, Stattic (10 μM) and U0126 (5 μM).

    U0126 purchased from MCE. Usage Cited in: Cancer Lett. 2017 Feb 16;393:22-32.

    Effects of p38 MAPK inhibitor (SB203580), ERK inhibitor (U0126), JNK inhibitor (SP600125), caspase inhibitor (Z-VAD-FMK) and NAC on SGC-7901 and MGC-803 treated with DOX/VCPA combination treatment. VCPA pretreatment strategy is the same as above. SB203580 (20 μM), U0126 (10 μM), SP600125 (20 μM), Z-VAD-FMK (10 μM) and NAC (5 mM) are treated 2 h before DOX (2 μg/mL) added into the culture, respectively. MAPK pathway protein levels are determined.

    U0126 purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2017;2017:6175841.

    Involvements of MAPK signaling pathway in CPS-induced apoptosis in ALI cultures of sheep bronchial epithelial cells. Cells are pretreated with U0126 (an ERK1/2 inhibitor, 10 μM) for 1 h, followed by exposure to CPS (100 ng/mL) or MO (MOI = 30) for 48 h. Cell lysates are subjected to Western blotting analysis using indicated antibodies.

    U0126 purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2017;2017:6175841.

    Involvements of MAPK signaling pathway in CPS-induced apoptosis in ALI cultures of sheep bronchial epithelial cells. Cells are pretreated with SP600125 (a JNK inhibitor, 20 μM) for 1 h, followed by exposure to CPS (100 ng/mL) or MO (MOI = 30) for 48 h. Cell lysates are subjected to Western blotting analysis using indicated antibodies.

    U0126 purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2017;2017:6175841.

    Involvements of MAPK signaling pathway in CPS-induced apoptosis in ALI cultures of sheep bronchial epithelial cells. Cells are pretreated with SB203580 (a P38 inhibitor, 20 μM) for 1 h, followed by exposure to CPS (100 ng/mL) or MO (MOI = 30) for 48 h. Cell lysates are subjected to Western blotting analysis using indicated antibodies.

    U0126 purchased from MCE. Usage Cited in: J Mol Cell Cardiol. 2015 Dec;89(Pt B):268-79.

    Dose response of MAPK and Akt inhibitors on cardiac fibroblast-derived exosomes (Exo)-induced activation of MAPKs and Akt. Neonatal rat cardiomyocytes are treated with or without Exo (50 μg/mL), U0126, SP600125, MK-2206, and SB023580 for 20 min and subjected to Western blot analysis. The results are from 4 separate experiments.

    U0126 purchased from MCE. Usage Cited in: Oncotarget. 2017 May 16;8(20):33807-33826.

    U0126 inhibits ERK1/2 activation in the kidney of hyperuricemic rats. Rat model of HN is established by feeding with adenine and potassium oxonate daily. In some rats, U0126 are simultaneously administrated intraperitoneally. After 28 days, the kidneys are taken for immunoblot analysis of p-ERK1/2, ERK1/2 or GAPDH.

    U0126 purchased from MCE. Usage Cited in: Free Radic Biol Med. 2017 Jul 9;112:49-59.

    Cells are pre-treated with ERK (U1026) and p38 (SB203580) inhibitors, followed by GL-V9 treatment for 24 h. Western blot is performed to analyze NAG-1 expression.

    U0126 purchased from MCE. Usage Cited in: Front Mol Neurosci. 2017 Mar 13;10:51.

    GSK-J1 impaired zebrafish hair cell regeneration. 5 dpf larvae are treated with 400 μM Neomycin for 1 h followed by GSK-J1 exposure for 24 in the presence of BrdU. GSK-J1 significantly reduces the numbers of myosinVI-positive (green) hair cells and BrdU-positive (red) replicating cells.

    U0126 purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2017;2017:7426458.

    Representative immunoblot analysis of p53, p16, p21, and retinoblastoma protein (Rb) in NP cells.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    U0126 is a non-ATP competitive MEK inhibitor, with IC50 of 70 nM and 60 nM for MEK1 and MEK2, respectively.

    IC50 & Target

    IC50: 70/60 nM (MEK1/2)[1]

    In Vitro

    Treatment with U0126 efficiently reduces progeny virus titers of all tested strains in A549 cells. While nM concentrations of U0126 are efficient to reduce H1N1v and H5N1 (MB1), μM concentrations of U0126 are required to reduce the virus titer of H5N1 (GSB) and H7N7. The EC50 values for U0126 against H1N1v are 1.2±0.4 μM in A549 cells and 74.7±1.0 μM in MDCKII cells[2].Rat hepatocarcinoma cells (FAO) stimulated by fetal calf serum (FCS) exhibits a significant proportion in S phase (32.62%) whereas U0126 strongly decreases the proportion of cells in S phase (9.92%) and increases the proportion of cells in G0-G1 phase and to a lesser extent in G2/M[3].

    In Vivo

    Mice are treated daily with U0126 (i.p., 10.5 mg/kg). In control experiment, tumor sizes are constant or slightly increase all over the kinetic. At the opposite, in all U0126 experiments, engraftment and early tumor growth are significantly decreased. Furthermore, a 60-70% reduction in the volume of tumors treated with U0126 is obtained 9 days after injection and thereafter[3]. Rats are subjected to 120?minutes transient middle cerebral artery occlusion (tMCAO) and thereafter treated with the U0126 (i.p., 30 mg/kg) at 0 and 24 hours of reperfusion. After treatment with U0126, the vasoconstriction to S6c is markedly reduced[4].

    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.3443 mL 11.7217 mL 23.4434 mL
    5 mM 0.4689 mL 2.3443 mL 4.6887 mL
    10 mM 0.2344 mL 1.1722 mL 2.3443 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [2]

    U0126 is dissolved in DMSO (10 mM) and stored, and then diluted with appropriate media (DMSO 1%) before use[2].

    A549 and MDCK II cells are seeded in 96-well culture plates at a density of 8×104 cells per well in minimal essential medium (MEM) containing 10% heat-inactivated fetal calf serum (FCS), 100 U/mL Penicillin, 100 mg/mL Streptomycin. Cells are incubated at 37°C with 5% CO2 overnight. Thereafter, cells are washed twice with PBS. MEM containing different concentrations of U0126 (0.001-1000 μM) is added to the cells. After addition of U0126, cells are incubated further for 48 h at 37°C and 5% CO2. Then, cells are fixed by incubation for 30 min at 4°C with 100 μL 4% paraformaldehyde (PFA). Adding 100 μL crystal violet for 30 min at room temperature stained viable cells. After staining, plates are washed and dried. For the extraction of crystal violet from viable cells 100 μL of 100% methanol is added to each well. After incubation for 30 min at room temperature, the extinction is measured with an enzyme-linked immunosorbent assay (ELISA) reader at OD=490 nm. The percentage of cell viability after treatment with the antiviral compound is calculated[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3][4]

    U0126 is dissolved in DMSO.

    Mice[3]
    Athymic female nude mice (SWISS, nu/nu) are used. Prior to injection, FI cells are labeled with a stable fluorescent dye molecule, DiA at 10 μg/mL for 5 h at 37°C. After washing to remove free DiA, cells are trypsinized for inoculation (U0126 experiments) or transfection (RNAi experiments). Biliary epithelial cells are injected subcutaneously, at the indicated times, into the tibia of nude mice. In the chemical experiments, 3 h after inoculation, mice are treated with U0126 (10.5 mg/kg) daily by intraperitoneal injection. The length and width of each tumor are measured every day by using a caliper. The following formula is used to calculate tumor volumes=width2×length/2. Mice are killed at the end of experiment. Tumors are immediately frozen in liquid nitrogen.
    Rat[4]
    Twelve-week-old female Wistar rats (250 to 265 g) are used U0126 (30 mg/kg intraperitoneally) is injected at 0 and 24 hours of reperfusion after tMCAO based on the previous evaluation of the drug in male rats. Animals in study II are administered U0126 or vehicle and are killed 14 days after tMCAO. Experimental group assignments are randomized and blinded to the surgical experimenter. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    426.56

    Formula

    C₂₀H₂₂N₆OS₂

    CAS No.

    1173097-76-1

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 49 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 98.03%

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    Product Name:
    U0126
    Cat. No.:
    HY-12031
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