1. MAPK/ERK Pathway Stem Cell/Wnt Immunology/Inflammation Autophagy
  2. MEK ERK Aryl Hydrocarbon Receptor Autophagy
  3. PD98059

PD98059 est un inhibiteur de MEK puissant et sélectif avec un IC50 de 5 µM. PD98059 se lie à la forme inactive de MEK, empêche ainsi l'activation de MEK1 (IC50 de 2-7 µM) et MEK2 (IC50 de 50 µM) par des kinases en amont. PD98059 est un ligand pour le récepteur arylhydrocarboné (AHR), et supprime la liaison TCDD (IC50 de 4 μM) et la transformation de AHR (IC50 de 1 μM). PD98059 inhibe également l'autophagie.

PD98059 ist ein potenter und selektiver MEK-Inhibitor mit einem IC50 von 5 µM. PD98059 bindet an die inaktive Form von MEK und verhindert dadurch die Aktivierung von MEK1 (IC50 von 2-7 µM) und MEK2 (IC50 von 50 µM) durch vorgeschaltete Kinasen. PD98059 ist ein Ligand für den Arylkohlenwasserstoff-Rezeptor (AHR) und unterdrückt die TCDD-Bindung (IC50 von 4 μM) und die AHR-Transformation (IC50 von 1 μM). PD98059 hemmt auch die Autophagie.

PD98059 is a potent and selective MEK inhibitor with an IC50 of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC50 of 2-7 µM) and MEK2 (IC50 of 50 µM) by upstream kinases. PD98059 is a ERK1/2 signaling inhibitor. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC50 of 4 μM) and AHR transformation (IC50 of 1 μM). PD98059 also inhibits Mycobacterium bovis Bacillus CalmetteGuerin (BCG)-induced autophagy.

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

PD98059 Chemical Structure

PD98059 Chemical Structure

CAS No. : 167869-21-8

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 66 In-stock
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50 mg USD 132 In-stock
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Customer Review

Based on 303 publication(s) in Google Scholar

Top Publications Citing Use of Products

285 Publications Citing Use of MCE PD98059

IF
WB

    PD98059 purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2023 Feb 1;116:109763.  [Abstract]

    PD98059 (0,10,30 μM; 24 h) inhibits the expression of p-ERK, Nrf2, Hif-1α, and IL-17D in NCM460 cells.

    PD98059 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2019 Apr;22:101133.  [Abstract]

    The effects of inhibitor PD98059 on the phosphorylated-ERK1/2, total ERK1/2, Thr181-phosphorylated tau, Thr205-phosphorylated tau, total tau and ROS production in different groups with or without Aβ25-35/FGF21.

    PD98059 purchased from MedChemExpress. Usage Cited in: Mol Cell. 2018 Feb 1;69(3):480-492.e7.  [Abstract]

    ERK is important for Nur77 phosphorylation. MV3 cells are pretreated with different kinase inhibitors (PD98059, 40 μM; SB202190, 20 μM; SP600125, 25 μM) before 3 hr of glucose starvation.

    PD98059 purchased from MedChemExpress. Usage Cited in: Cell Mol Life Sci. 2018 Mar;75(6):1117-1132.  [Abstract]

    Sertoli cells (SC) are pretreated with the PD98059 for 1 h followed by a 24-h treatment with MC-LR. Expression levels of MMP-8, c-Jun, c-Fos, p-ERK, ERK, p-JNK, and JNK are determined by western blotting.

    PD98059 purchased from MedChemExpress. Usage Cited in: Cell Mol Life Sci. 2018 Jul;75(14):2627-2641.  [Abstract]

    RAW264.7 macrophages are pre-treated with the inhibitor of ERK, JNK, P38, P65, and AKT signal pathway.Western blot analyzes the non- and phosphorylation of ERK, JNK, P38, P65, and AKT.

    PD98059 purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2018 Feb;98:36-44.  [Abstract]

    Resveratrol (RES) inhibits epithelial-mesenchymal transition (EMT) and extracellular matrix (ECM) remodeling of renal cell carcinoma (RCC) cells via the Akt and ERK1/2 signaling pathway. RCC cell lines are treated with RES (0, 50, 100 μM) and 50 μM PD98059 for 24 h. Levels of Akt, p-Akt, ERK1/2, p-ERK1/2 proteins are examined by Western blot.

    PD98059 purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2018 Mar;12(3):305-321.  [Abstract]

    Western blot analysis of the expression level of EGFR, Sp1, total and phosphorylated Erk1/2 proteins in cell lysates from two breast cancer cells pretreated with PD98059 and then stimulated with TGF-β for the indicated times

    PD98059 purchased from MedChemExpress. Usage Cited in: J Agric Food Chem. 2018 Jun 27;66(25):6317-6325.  [Abstract]

    HepG2 cells are pre-incubated with 20 µM SB203580, SP600125 and PD98059 for 1 h and then treated with tangeretin(20µM) for 24 h.

    PD98059 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Feb 12;8(1):2848.  [Abstract]

    The expression of EGFR, p-EGFR, ERK, p-ERK and FOS in four groups (from left to right: 50 μM PD98059, 30 min; control; pretreatment with 50 μM PD98059, 30 min, then intervened with 0.1 mg/L BER 15 min; 0.1 mg/L BER for 15 min) are examined using western blot.

    PD98059 purchased from MedChemExpress. Usage Cited in: Toxicology. 2018 Dec 1;410:222-230.  [Abstract]

    SH-SY5Y cells are pretreated with MEK inhibitor PD98059 (10 μM) for 1 h, then incubated with NaF (60 mg/L) for 24 h. Representative images of western blotting for BDNF, TrkB and p-ERK1/2 in SH-SY5Y cells.

    PD98059 purchased from MedChemExpress. Usage Cited in: Mol Cell Biochem. 2018 Feb;439(1-2):117-129.  [Abstract]

    Protein expression levels of E-cadherin N-cadherin, p-ERK, ERK, TGF-β1, p-Smad2, and p-Smad3 in each group are analyzed by western blotting.

    PD98059 purchased from MedChemExpress. Usage Cited in: World J Gastroenterol. 2018 Feb 21;24(7):819-832.  [Abstract]

    HSCs are pretreated with AICAR (500 μM), LY294002 (20 μM), PD98059 (10 μM), or Rapamycin (100 nM) for 2 h and then incubated with or without CoCl2 (150 μM) for 12 h. Expression levels of HIF-1α and VEGF are measured by Western blot analysis;

    PD98059 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Jan 1;495(1):781-786.  [Abstract]

    Representative images of migrated cells. HUVECs are pretreated with PD98059 (10 μM), SCH772984 (500 nM) or mock control for 2 h, and seeded in upper chambers of transwell inserts. VEGF (100 ng/ml), Scg3 (1 μg/ml) or PBS in medium with reduced FBS is added to bottom chambers in the presence or absence of the inhibitor. After culturing for 4 or 20 h, cells migrated to the lower surface of transwell membrane are stained with DAPI.

    PD98059 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Dec 9;507(1-4):253-259.  [Abstract]

    The expression of p-ERK1/2, ERK1/2, AGCAN and COL2 detected by Western blot in degenerated NP cells treated with or without rhLIF (100 ng/ml) and PD98059 (0 μM, 25 μM, 50 μM) for 48 h.

    PD98059 purchased from MedChemExpress. Usage Cited in: Mol Immunol. 2017 Jul;87:161-170.  [Abstract]

    Effect of TLR2 on autophagy activation via ERK1/2 signaling pathway activation in MG-infected RAW264.7 cells. RAW264.7 cells transfected with TLR2 siRNA/control siRNA is then infected with MG for 30 min prior to PD98059. The expression levels of Beclin1, LC3-II/I, p-JNK, p-ERK1/2 and p-p38 are examined by Western blot.

    PD98059 purchased from MedChemExpress. Usage Cited in: Hum Mol Genet. 2017 Sep 15;26(18):3553-3563.  [Abstract]

    Immunofluorescence analysis for expression of the I-cell marker ΔNP63 on proximal sections of ureters explanted from E12.5 wildtype (control) embryos and cultured for 6 d in the presence of solvent (DMSO) (A), the AKT inhibitor (AKT-i) MK2206 (B), the P38 inhibitor (P38-i) SB203580 (C), the ERK1/2 inhibitor (ERK1/2-i) PD98059 (D) or combinations as indicated (E and F).

    PD98059 purchased from MedChemExpress. Usage Cited in: Exp Ther Med. 2017 Apr;13(4):1353-1359.  [Abstract]

    Hippocampal neuron lysates are subjected to western blotting to evaluate Nrf2 levels and the phosphorylation of ERK in the presence and absence of PD98059.

    PD98059 purchased from MedChemExpress. Usage Cited in: Biomed Res. 2017; 28 (8): 3383-3386

    Effects of various protease inhibitors on HO-1 and P-gp protein expressions.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    PD98059 is a potent and selective MEK inhibitor with an IC50 of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC50 of 2-7 µM) and MEK2 (IC50 of 50 µM) by upstream kinases. PD98059 is a ERK1/2 signaling inhibitor. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC50 of 4 μM) and AHR transformation (IC50 of 1 μM). PD98059 also inhibits Mycobacterium bovis Bacillus CalmetteGuerin (BCG)-induced autophagy[1][2][3].

    IC50 & Target[1][3]

    MEK1

    2-7 μM (IC50)

    MEK2

    50 μM (IC50)

    ERK1

     

    ERK2

     

    Autophagy

     

    In Vitro

    PD98059 (20 μM; 24 hours) causes G1-phase cell cycle arrest in OCI-AML-3 cells[4].
    PD98059 (10 μM; 22 hours) results in concentration-dependent reductions in the dually phosphorylated forms of ERK1 and ERK2[1]. PD98059 both prevents ERK activation and blocks formation of TDP-43 and HuR-positive SGs[7].

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

    Cell Cycle Analysis[4]

    Cell Line: OCI-AML-3 cells
    Concentration: 20 μM
    Incubation Time: 24 hours
    Result: Caused G1-phase cell cycle arrest.

    Western Blot Analysis[1]

    Cell Line: MCF10A-Neo, MCF10ANeoT cells
    Concentration: 10 μM
    Incubation Time: 22 hours
    Result: Phosphorylated ERK forms were almost completely eliminated in both cell lines.
    In Vivo

    PD98059 (10 mg/kg; i.p.; 1 and 6 hours after Zymosan) significantly reduces the level of p-ERK1/2 in zymosan-injected mice[3].

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

    Animal Model: Male CD mice[3]
    Dosage: 10 mg/kg
    Administration: Intraperitoneal injection; 1 and 6 hours after Zymosan
    Result: Significantly reduced the level of p-ERK1/2.
    Molecular Weight

    267.28

    Formula

    C16H13NO3

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C1C=C(OC2=CC=CC=C21)C3=CC=CC(OC)=C3N

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, protect from light

    *In solvent : -80°C, 1 years; -20°C, 6 months (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 33.33 mg/mL (124.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.7414 mL 18.7070 mL 37.4139 mL
    5 mM 0.7483 mL 3.7414 mL 7.4828 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, 1 years; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

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    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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    90% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (7.78 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  50% PEG300    50% Saline

      Solubility: 10 mg/mL (37.41 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
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    %
    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).

    *In solvent : -80°C, 1 years; -20°C, 6 months (protect from light)

    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: 99.96%

    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, 1 years; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.7414 mL 18.7070 mL 37.4139 mL 93.5349 mL
    5 mM 0.7483 mL 3.7414 mL 7.4828 mL 18.7070 mL
    10 mM 0.3741 mL 1.8707 mL 3.7414 mL 9.3535 mL
    15 mM 0.2494 mL 1.2471 mL 2.4943 mL 6.2357 mL
    20 mM 0.1871 mL 0.9353 mL 1.8707 mL 4.6767 mL
    25 mM 0.1497 mL 0.7483 mL 1.4966 mL 3.7414 mL
    30 mM 0.1247 mL 0.6236 mL 1.2471 mL 3.1178 mL
    40 mM 0.0935 mL 0.4677 mL 0.9353 mL 2.3384 mL
    50 mM 0.0748 mL 0.3741 mL 0.7483 mL 1.8707 mL
    60 mM 0.0624 mL 0.3118 mL 0.6236 mL 1.5589 mL
    80 mM 0.0468 mL 0.2338 mL 0.4677 mL 1.1692 mL
    100 mM 0.0374 mL 0.1871 mL 0.3741 mL 0.9353 mL
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      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.

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