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  3. PD98059

PD98059 

Cat. No.: HY-12028 Purity: 99.33%
Handling Instructions

PD98059 is a selective, cell permeable inhibitor of the MEK. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC50=2-7 µM) and MEK2 (IC50=50 µM) by upstream kinases. PD98059 causes G1 arrest by blocking p53-dependent p21 induction.

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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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 132 In-stock
Estimated Time of Arrival: December 31
100 mg USD 228 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 74 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE PD98059

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

    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 MCE. Usage Cited in: Mol Immunol. 2017 Jul;87:161-170.

    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 MCE. Usage Cited in: Biomed Res. 2017; 28 (8): 3383-3386

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

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

    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 MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Jan 1;495(1):781-786.

    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 MCE. Usage Cited in: Cell Mol Life Sci. 2018 Mar;75(6):1117-1132.

    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 MCE. Usage Cited in: Biomed Pharmacother. 2018 Feb;98:36-44.

    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 MCE. Usage Cited in: Mol Oncol. 2018 Mar;12(3):305-321.

    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 MCE. Usage Cited in: Hum Mol Genet. 2017 Sep 15;26(18):3553-3563.

    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 MCE. Usage Cited in: Cell Mol Life Sci. 2018 Jul;75(14):2627-2641.

    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 MCE. Usage Cited in: Mol Cell. 2018 Feb 1;69(3):480-492.e7.

    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 MCE. Usage Cited in: Sci Rep. 2018 Feb 12;8(1):2848.

    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 MCE. Usage Cited in: World J Gastroenterol. 2018 Feb 21;24(7):819-832.

    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 MCE. Usage Cited in: J Agric Food Chem. 2018 Jun 27;66(25):6317-6325.

    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 MCE. Usage Cited in: Toxicology. 2018 Dec 1;410:222-230.

    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 MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Dec 9;507(1-4):253-259.

    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 MCE. Usage Cited in: Redox Biol. 2019 Apr;22:101133.

    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.

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    Description

    PD98059 is a selective, cell permeable inhibitor of the MEK. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC50=2-7 µM) and MEK2 (IC50=50 µM) by upstream kinases. PD98059 causes G1 arrest by blocking p53-dependent p21 induction.

    IC50 & Target[1]

    MEK1

    2-7 μM (IC50)

    MEK2

    50 μM (IC50)

    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].

    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].

    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.

    167869-21-8

    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, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 16 mg/mL (59.86 mM; Need ultrasonic and warming)

    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
    10 mM 0.3741 mL 1.8707 mL 3.7414 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

      Solubility: ≥ 2.5 mg/mL (9.35 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.5 mg/mL (9.35 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.33%

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    Product Name:
    PD98059
    Cat. No.:
    HY-12028
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