1. MAPK/ERK Pathway
    Autophagy
  2. MEK
    Autophagy

PD98059 

Cat. No.: HY-12028 Purity: 99.45%
Data Sheet SDS Handling Instructions

PD98059 is a MEK inhibitor with IC50 of 5 μM, also suppresses TCDD binding to the aryl hydrocarbon receptor (AHR) with IC50 of 4 μM.

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 USD 66 In-stock
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Customer Review

    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: Biomedical Research 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. 2017 Aug 12.

    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: Br J Cancer. 2017 Sep 26;117(7):974-983.

    The effect of the AKT inhibitor MK2206 (10 μM) on the expression levels of phosphor-AKT, AKT, and STMN1 in TKI-pretreated NCI-H460 cells. β-actin is used as a loading control.

    PD98059 purchased from MCE. Usage Cited in: Cell Mol Life Sci. 2017 Oct 25.

    Sertoli cells (SC) are pretreated with BAY11-7082 at 2 μM for 1 h, followed by the addition of MC-LR into the culture medium. Expression of p-p65 and MMP-8 is measured by western blotting.

    PD98059 purchased from MCE. Usage Cited in: Cell Mol Life Sci. 2017 Oct 25.

    Sertoli cells (SC) are pretreated with LY294002 at 20 μM for 1 h followed by a 24-h treatment with MC-LR. Expression levels of p-p65 and MMP-8 are detected by western blotting.

    PD98059 purchased from MCE. Usage Cited in: Cell Mol Life Sci. 2017 Oct 25.

    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: Cell Mol Life Sci. 2017 Oct 25.

    Sertoli cells (SC) are pretreated with the SP600125 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. 2017 Dec 11;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. 2017 Dec 7.

    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: Mol Oncol. 2017 Dec 7.

    Western blot analysis of EGFR, total and phosphorylated Smad3, total and phosphorylated ERK protein expression in cell lysates from two breast cancer cells pretreated with SB431542 and then stimulated with TGF-β for the indicated times.

    PD98059 purchased from MCE. Usage Cited in: Mol Oncol. 2017 Dec 7.

    Western blot analysis of total and phosphorylated EGFR expression in two breast cancer cells pretreated with different concentration Erlotinib for 4h.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    PD98059 is a MEK inhibitor with IC50 of 5 μM, also suppresses TCDD binding to the aryl hydrocarbon receptor (AHR) with IC50 of 4 μM.

    IC50 & Target

    IC50: 5 μM (MEK)[1]

    In Vitro

    Concentrations of PD98059 of ≤20 μM are not cytotoxic to cultured MCF10A, MCF10A-Neo, and MCF10A-NeoT cells. However, PD98059 is weakly cytostatic to all three lines at concentrations of ≥10 μM. Treatment of MCF10A-Neo and MCF10A-NeoT cultures with concentrations of PD98059 up to 20 μM for 2-22 hr does not alter the total ERK content. However, treatment with PD98059 does result in concentration-dependent reductions in the dually phosphorylated forms of ERK1 and ERK2. Within 2 hr of a 10-μM treatment, phosphorylated ERK contents are reduced ~74% and ~86% in MCF10A-Neo and MCF10A-NeoT cultures, respectively (IC50=1 μM). Within 22 hr of treatment, phosphorylated ERK forms are almost completely eliminated in both cell lines[1]. PD98059 (PD 098059) prevents the activation of MAPKK1 by Raf or MEK kinase in vitro at concentrations (IC50=2-7 μM). PD98059 inhibits both the activation and phosphorylation of MAPKK1 in vitro by either c-Raf or MEK kinase with IC50 values of 4±2 μM. Incubation of Swiss 3T3 cells with PD98059 (50 μM) suppressed by 80-90% the activation of MAPKK induced by each agonist, but the activation of c-Raf is enhanced 2-3-fold[2].

    In Vivo

    The treatment of mice with PD98059 significantly reduces the level of p-ERK1/2. Moreover, a significant increase in the phospho-p38 expression is observed in Zymosan-treated mice at 18 h after Zymosan administration compared to the sham-operated mice. The treatment with PD98059 significantly reduces the p38 expression[3]. Repeated treatment with PD98059 attenuates mechanical allodynia measured by the von Frey test three (18.0 g±0.8, n=10) and seven (20.21 g±0.67, n=26) days after CCI in comparison to the vehicle-treated CCI-exposed rats (15.1 g±1.3, n=7 and 14.21 g±0.44, n=28, respectively). Repeated injection of PD98059 diminishes thermal hyperalgesia, as is evaluated by the cold plate test, three (17.5 s±2.1, n=10) and seven (25.54 s±1.03, n=26) days following CCI compared to vehicle-treated CCI-exposed rats (11.5 s±1.8, n=7 and 11.4 s±0.88, n=28, respectively)[4].

    References
    Preparing Stock Solutions
    Concentration Volume 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.
    Kinase Assay
    [1]

    Kinase reactions are performed in 50 μL reaction volumes and contain 50 mM Tris, pH 7.4, 10 mM MgCl2, 2 mM EGTA, 10 μM ATP (containing 1 μCi of 3000 Ci/mmol [γ-32P]ATP), 7.6 μg of GST-MEK1, 7.2 μg of GST-ERK1, and 20 μg of MBP. PD98059 and other flavonoids are added to the reactions mixtures immediately after the addition of GST-MEK1 but before the addition of GST-ERK1 and ATP. Control reactions contain ERK1 and MBP but no MEK. Reaction mixtures are incubated at 30°C for 15 min before being stopped by the addition of Laemmli’s SDS sample buffer. Proteins are separated on SDS-15% polyacrylamide gels. After vacuum drying of the gel, radioactivity is detected by autoradiography on X-ray film or phosphoimaging using a BioRad GS-525 Molecular Imager[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    PD98059 is dissolved in DMSO and stored, and then diluted with appropriate media (DMSO <0.1%) before use[1].

    The MCF10A, MCF10A-Neo, and MCF10A-NeoT cell lines are used. Subconfluent cultures are treated with PD98059 (0-100 μM). Viability of cells after treatment is assessed by ability to exclude trypan blue. Cultures earmarked for RNA isolation are washed twice with phosphate-buffered saline (2.7 mM KCl, 1.5 mM KH2PO4, 137 mM NaCl, 8 mM Na2HPO4, pH 7.2) at harvesting and stored at -80°C[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3][4]

    PD98059 is prepared in non-pyrogenic saline (0.9% NaCl) (Mice)[3].
    PD98059 is dissolved in 75% DMSO (Rats)[4].

    Mice[3]
    Male CD mice (20-22 g) are randomly allocated into the following groups: 1. Zymosan+DMSO group. Mice are treated intraperitoneally (i.p.) with Zymosan (500 mg/kg, suspended in saline solution) and with the vehicle for PD98059 (10% DMSO, v/v) i.p. 1 and 6 h after Zymosan administration (N=10). 2. PD98059 group. Identical to the Zymosan+DMSO group but are administered PD98059 (10 mg/kg, i.p. bolus) at 1 and 6 h after Zymosan (N=10) instead of DMSO. 3. Sham+DMSO group. Identical to the Zymosan+DMSO group but are administered saline solution instead of Zymosan (N=10). 4. Sham+PD98059 group. Identical to Sham+DMSO group, except for the administration of PD98059 (10 mg/kg i.p. bolus) 1 and 6 h after saline administration (N=10).
    Rats[4]
    The rats (male Wistar, 300-350 g) are used. The PD98059 (2.5 μg/5 μL, i.t.) is single or repeated preemptively administered 16 h and 1 h before CCI and then once daily for 7 days. The Vehicle-treated CCI-exposed rats receive 75% DMSO according to the same schedule. There is no significant difference in pain behavior between no-treated and V(DMSO)-treated CCI-exposed rats. This method of PD98059 or vehicle administration is used throughout the study and is referred to in the text as “repeated administration”. At day 7th after CCI 30 min after PD98059 administration tactile allodynia is measured using von Frey test and thermal hyperalgesia is conducted using cold plate test. Additionally, at day 7th after CCI the vehicle-treated and PD98059-treated rats receive a single i.t. vehicle, Morphine (2.5 μg/5 μL) or Buprenorphine (2.5 μg/5 μL) injection 30 min after PD98059, and then 30 min later the von Frey and/or cold plate tests are repeated. Since the dose of morphine 2.5 μg/5 μL in naive rats produces maximal analgesic effect in tail-flick test. Lower dose of Morphine are used for co-administration experiments, so that observing the possible enhancement of opioid effectiveness. The vehicle-treated and PD98059-treated naive rats (uninjured rats) receive a single i.t. vehicle, Morphine (0.5 μg/5 μL) or Buprenorphine (2.5 μg/5 μL) injection 30 min after PD98059, and then 30 min later the tail flick test is performed. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    267.28

    Formula

    C₁₆H₁₃NO₃

    CAS No.

    167869-21-8

    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: 16 mg/mL; H2O: < 0.01 mg/mL

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

    Purity: 99.45%

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