2. MAPK/ERK Pathway Autophagy Anti-infection
  3. MEK Autophagy Mitophagy Influenza Virus
  4. U0126

U0126 is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC50s of 72 nM and 58 nM, respectively. U0126 is an autophagy and mitophagy inhibitor.

For research use only. We do not sell to patients.

U0126 Chemical Structure

U0126 Chemical Structure

CAS No. : 109511-58-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 132 In-stock
Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Solid
1 mg USD 48 In-stock
5 mg USD 120 In-stock
10 mg USD 192 In-stock
25 mg USD 365 In-stock
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Customer Review

Based on 397 publication(s) in Google Scholar

Other Forms of U0126:

U0126 Related Antibodies

Top Publications Citing Use of Products

360 Publications Citing Use of MCE U0126

WB
RT-PCR
IHC

    U0126 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2023 Mar 7;115489.  [Abstract]

    U0126 (20 uM; pretreat for 2 h) rescues the loss of UHRF1/DNMT1 expression and the increase of E-Cadherin expression that induced by Lenvatinib in Huh7 cells.

    U0126 purchased from MedChemExpress. Usage Cited in: Mol Cell Endocrinol. 2023 Feb 17;111891.  [Abstract]

    U0126 (10 uM; pre-treate for 1 h) attenuates IL-1-induced upregulation of COX-2 expression in KGN cells.

    U0126 purchased from MedChemExpress. Usage Cited in: Cancer Res. 2019 Sep 1;79(17):4466-4479.  [Abstract]

    Western blot and IHC analyses for p-ERK1/2 in lung tissues after vehicle or U0126 treatment.

    U0126 purchased from MedChemExpress. Usage Cited in: Am J Physiol Renal Physiol. 2019 Apr 1;316(4):F660-F673.  [Abstract]

    Western analysis of α-SMA, Collagen I and E-cadherin protein expression in the treatment of U0126 with different concentrations.

    U0126 purchased from MedChemExpress. Usage Cited in: Am J Physiol Renal Physiol. 2019 Apr 1;316(4):F660-F673.  [Abstract]

    Western analysis of Vimentin, E-cadherin and Snail1 protein expression with or without the treatment of U0126.

    U0126 purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2019 Jan;120(1):321-331.  [Abstract]

    U0126 enhances the negative effect of Fsk-IBMX on the development of glioma stem cells (GSCs).

    U0126 purchased from MedChemExpress. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2019 Apr 1;51(4):365-374.  [Abstract]

    MAPKs inhibitors suppress LPS-induced COX-2 expression and AKT1 phosphorylation. RAW264.7 cells are pretreated for 1 h with U0126, SB202190, SP600125 alone, or all the three inhibitors, respectively, and then exposed to 40 ng/ml LPS for 30 min or 12 h. The phosphorylated protein kinases and COX-2 expression are detected by western blot analysis using their corresponding antibodies.

    U0126 purchased from MedChemExpress. Usage Cited in: Blood. 2018 Jul 12;132(2):210-222.  [Abstract]

    Phosphorylation of p-ERK1/2 and p-Akt in MKs pretreated with 0.5 μM NVP-ADW742, 10 μM U0126 or 20 μM LY294002 followed by rhIGF-1 treatment for 15 minutes.

    U0126 purchased from MedChemExpress. Usage Cited in: Biomaterials. 2018 Sep;178:95-108.  [Abstract]

    U0126 effectively inhibits the phosphorylation of ERK, leading to the inhibition of IL-10 production.

    U0126 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2018 Aug 28;430:201-214.  [Abstract]

    Inhibition of ERK suppresses N-cadherin expression. CD146WT or CD146KO MEFs are stimulated with or without TGF-β1 (10 ng/mL) for 24 h in the presence or absence of U0126 (2 μM). The expression and activation of ERK and the expression of E-cadherin and N-cadherin is assessed by immunoblotting.

    U0126 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2018 Oct 19;15(1):291.  [Abstract]

    Blocking the three MAPK signaling pathways through specific inhibitors (U0126; SB202190; and SP600125) significantly decrease the infection-induced neuroinflammatory response via real-time PCR analysis.

    U0126 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2018 Oct 19;15(1):291.  [Abstract]

    Blocking the three MAPK signaling pathways through specific inhibitors (U0126; SB202190; and SP600125) significantly decrease the infection-induced neuroinflammatory response via real-time PCR analysis.

    U0126 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2018 Jun 15;15(1):184.  [Abstract]

    Representative immunoblots of total lysates from BV2 cells treated with MPP+or/and U0126 (10 μM), SP600125 (SP, 10 μM) and SB203580 (SB, 10 μM) using the antibodies against DICER.

    U0126 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Oct 3;9(10):1015.  [Abstract]

    Representative western blot images are showing the LC3, and the phosphorylated and total protein expression of Akt and ERK1/2 after treatment with H2O2 in the presence and absence of MK2206 (5 μM) and U0126 (25 μM).

    U0126 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Feb 15;9(3):269.  [Abstract]

    WB is used to detect the effect of EGF treatment on the expression of YAP with the inhibitors of EGFR or its downsream members.

    U0126 purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2018 Mar 15;42:152-163.  [Abstract]

    Cells are pretreated with SP600125 (20 μM), SB203580 (20 μM) or U0126 (20 μM) in presence or absence of KLA, then incubated with LPS (1 μg/mL) for certain time. Cell lysates are subjected to western blot.

    U0126 purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2018 Feb 19;100:417-425.  [Abstract]

    HaCaT cells are pre-incubated with Compound C (CC) (10 μM) and U0126 (10 μM), pharmacological inhibitors of AMPKα, ERK, respectively, for 1 h before treatment with DA8 and DA14 (DAs).

    U0126 purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

    As for both 0 g and 3 g groups, the p-p38&p38 is downregulated by inhibitors SB203580, SP600125, and U0126.

    U0126 purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

    The protein level of MMP-9 is downregulated by inhibitors SB203580, SP600125, and U0126.

    U0126 purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

    As for both 0 g and 3 g groups, the p-JNK1&JNK1 is downregulated by inhibitors SB203580, SP600125, and U0126.

    U0126 purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

    The protein levels of IL-1β and TNF-α are sharply downregulated by the addition of inhibitors SB203580, SP600125, and U0126.

    U0126 purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

    As for both 0 g and 3 g groups, the p-ERK1/2/ERK1/2 is notably reduced by inhibitors SB203580, SP600125, and U0126.

    U0126 purchased from MedChemExpress. Usage Cited in: Front Immunol. 2018 Dec 7;9:2854.  [Abstract]

    Neutrophils are pretreated with inhibitor of p38 MAPK (SB203580) and ERK1/2 (U0126), and the cells are then incubated with either SS2 ZY05719 or PMA for 3 h. Immunofluorescence is performed.

    U0126 purchased from MedChemExpress. Usage Cited in: Reprod Biol Endocrinol. 2018 May 31;16(1):55.  [Abstract]

    Western blot analysis of claudin 5, occludin and ZO-1 in TM4 cells, cells are treated with 100 nM Leptin or pre-treated with different inhibitors following a 100 nM Leptin treatment.

    U0126 purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2018 Sep 19.  [Abstract]

    Western blot shows the expression of p-ERK and MMP13 with the treatment of U0126 and CCL17.

    U0126 purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2018 Jun;17(6):7595-7602.  [Abstract]

    Representative images show the expression levels of α SMA, calponin and osteopontin (OPN) protein.

    U0126 purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2018;50(4):1522-1534.  [Abstract]

    Western analysis of effect of U0126 on Nell-1-induced changes in p-ERK, Runx2, OPG and Col-I protein expression in MC3T3-E1 preosteoblasts on Ti surfaces.

    U0126 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2017 Feb 16;393:22-32.  [Abstract]

    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 MedChemExpress. Usage Cited in: Free Radic Biol Med. 2017 Nov;112:49-59.  [Abstract]

    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 MedChemExpress. Usage Cited in: Cell Signal. 2017 Jan 16;32:48-58.   [Abstract]

    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 MedChemExpress. Usage Cited in: Cell Cycle. 2017 Apr 3;16(7):714-722.  [Abstract]

    Proliferation of OPCs by AST induced calcium signaling and phosphorylated ERK1/2. p-ERK levels decreased after Cx47 siRNA treatment and U0126-mediated ERK1/2 inhibition. The results of Western blotting show that U0126 causes a marked decrease in ERK1/2 phosphorylation

    U0126 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 May 30;8(47):82027-82036.  [Abstract]

    U0126 and MEK162 block ERK activation (p-ERK1/2) in CZ415-treated U2OS cells.

    U0126 purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2017;2017:7426458.  [Abstract]

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

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

    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 MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2017;2017:6175841.  [Abstract]

    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 MedChemExpress. Usage Cited in: ACS Chem Neurosci. 2015 Jan 21;6(1):130-7.  [Abstract]

    U0126 protects PC12 cells against H2O2-induced cell death. Western blot of ERK phosphorylation demonstrates that the MEK inhibitors U0126, GSK1120212 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 MedChemExpress. Usage Cited in: J Mol Cell Cardiol. 2015 Dec;89(Pt B):268-79.  [Abstract]

    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.

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    • Biological Activity

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    • References

    • Customer Review

    Description

    U0126 is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC50s of 72 nM and 58 nM, respectively. U0126 is an autophagy and mitophagy inhibitor[1][2][3][4].

    IC50 & Target[1]

    MEK2

    60 nM (IC50)

    MEK1

    70 nM (IC50)

    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-EtOH 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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    U0126 Related Antibodies

    Cell Viability Assay[2]

    Cell Line: A549 and MDCK II cells.
    Concentration: 0.001-1000 μM.
    Incubation Time: 48 h.
    Result: The EC50 values for U0126 against H1N1v were 1.2 ± 0.4 μM in A549 cells and 74.7 ± 1.0 μM in MDCKII cells
    In Vivo

    Mice are treated daily with U0126-EtOH (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-EtOH experiments, engraftment and early tumor growth are significantly decreased. Furthermore, a 60-70% reduction in the volume of tumors treated with U0126-EtOH 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-EtOH (U0126; i.p., 30 mg/kg) at 0 and 24 hours of reperfusion. After treatment with U0126-EtOH, the vasoconstriction to S6c is markedly reduced[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Athymic female nude mice (SWISS, nu/nu)[3].
    Dosage: 10.5 mg/kg.
    Administration: Intraperitoneal injection daily.
    Result: Inhibited tumor growth.
    Animal Model: Twelve-week-old female Wistar rats (250 to 265 g) [4].
    Dosage: 30 mg/kg.
    Administration: Intraperitoneally.
    Result: The vasoconstriction to S6c is markedly reduced.
    Molecular Weight

    380.49

    Formula

    C18H16N6S2
    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    NC1=CC=CC=C1S/C(N)=C(C#N)/C(C#N)=C(N)/SC2=CC=CC=C2N
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (262.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.6282 mL 13.1409 mL 26.2819 mL
    5 mM 0.5256 mL 2.6282 mL 5.2564 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.57 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.57 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 98.45%

    COA (249 KB) HNMR (275 KB) LCMS (100 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.6282 mL 13.1410 mL 26.2819 mL 65.7048 mL
    5 mM 0.5256 mL 2.6282 mL 5.2564 mL 13.1410 mL
    10 mM 0.2628 mL 1.3141 mL 2.6282 mL 6.5705 mL
    15 mM 0.1752 mL 0.8761 mL 1.7521 mL 4.3803 mL
    20 mM 0.1314 mL 0.6570 mL 1.3141 mL 3.2852 mL
    25 mM 0.1051 mL 0.5256 mL 1.0513 mL 2.6282 mL
    30 mM 0.0876 mL 0.4380 mL 0.8761 mL 2.1902 mL
    40 mM 0.0657 mL 0.3285 mL 0.6570 mL 1.6426 mL
    50 mM 0.0526 mL 0.2628 mL 0.5256 mL 1.3141 mL
    60 mM 0.0438 mL 0.2190 mL 0.4380 mL 1.0951 mL
    80 mM 0.0329 mL 0.1643 mL 0.3285 mL 0.8213 mL
    100 mM 0.0263 mL 0.1314 mL 0.2628 mL 0.6570 mL
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    U0126 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    U0126109511-58-2U 0126U-0126MEKAutophagyMitophagyInfluenza VirusMitogen-activated protein kinase kinaseMAPKKMAP2KMitochondrial AutophagyInhibitorinhibitorinhibit

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