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PD98059

Catalog No.S1177 4 Review(s) 3 Product Citation(s)
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PD98059 Chemical Structure

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Biological Activity

PD 98059 is a highly selective inhibitor of MEK1 and MEK2 with IC50 values of 4 µM and 50 µM respectively[1–3] . PD98059 does not inhibit activation of other highly related dual-specificity protein kinases or the activity of over 18 other Ser/Thr protein kinases. At concentrations up to 100 µM, PD98059 does not inhibit activation of MKK3 or SEK (MKK4) as determined by measuring phosphorylation at its activation site. [1–3]

References on PD98059
  • [1] The Journal of Neuroscience September 15, 1998;18(18):7296–7305
  • [2] The Journal of Neuroscience June 1, 1998;18(11):4008–4021
  • [3] MOLECULAR AND CELLULAR BIOLOGY Apr. 1998;18:1946–1955
Molecular Weight (WM): 267.28
Formula:

C16H13NO3

CAS No.: 167869-21-8
Synonyms:
N/A
Dissolve in (25°C): DMSO ≥32mg/mL 
Water <1mg/mL 
Ethanol ≥3mg/mL 
Storage: 2 years-20°CPowder
1 week-4°Cin DMSO
1 month-80°in DMSO

Quality Control & MSDS

View current batch:
COA H-NMR HPLC

Research Area

MAPK >> MEK >> MEK Inhibitors
Notes:

Related Inhibitors

Recommended Screening Libraries

Selleck's high quality products have been used in several published research findings, including the following:

Inhibitors of MAPK Pathway ERK1/2 or p38 prevent the IL-1β-induced up-regulation of SRP72 Autoantigen in Jurkat Cells
Myeloid related proteins activate Toll-like receptor 4 in human acute coronary syndromes
Akt Determines Cell Fate Through Inhibition of the PERK-eIF2{alpha} Phosphorylation Pathway

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  • Click to enlarge

    T47D cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of  PD98059 for 24 hours.

     

     

  • T47D cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of  PD98059 for 24 hours.

     

     

  • Data independently produced by Dr. Zhang of Tianjin Medical University
    PD98059 purchased from Selleck


  • Click to enlarge

    effect of ERK1/2 inhibitor PD98059 (1, 5, and 10 M) on SRP72 protein expression was evaluated on Jurkat cells stimulated with rhIL-1. The cells were harvested at 0,120, and 240 min, and the protein expression was verified byWBusing antibodies against human SRP72, human SRP54 (nonphosphorylated SRP protein), and humanGAPDHas constitutive protein.Adecreased SRP72 expression at 10M and 240 min was found.

     

     

  • effect of ERK1/2 inhibitor PD98059 (1, 5, and 10 M) on SRP72 protein expression was evaluated on Jurkat cells stimulated with rhIL-1. The cells were harvested at 0,120, and 240 min, and the protein expression was verified byWBusing antibodies against human SRP72, human SRP54 (nonphosphorylated SRP protein), and humanGAPDHas constitutive protein.Adecreased SRP72 expression at 10M and 240 min was found.

     

     

  • Data from [The Journal of Biological Chemistry 2010.October;285:32824-32833]
    PD98059 purchased from Selleck


  • Click to enlarge

    C, effect of ERK1/2 inhibitor PD98059 (1, 5, and 10 M) was evaluated in SRP72-immunoprecipitated cell lysates. WB using anti-phosphoserine antibody showed a decreased SRP72 band when used as the inhibitor at concentrations of 1 M at 240 min, 5 M at 120 min, and 10 M at 120 and 240 min (lanes 3, 5, 8, and 9). D, results were analyzed and RUA illustrated, finding significant results at 1 M at 240 versus 0, 5 M at 120 versus 0, and 10 M at 120 versus 0 min.

     

     

  • C, effect of ERK1/2 inhibitor PD98059 (1, 5, and 10 M) was evaluated in SRP72-immunoprecipitated cell lysates. WB using anti-phosphoserine antibody showed a decreased SRP72 band when used as the inhibitor at concentrations of 1 M at 240 min, 5 M at 120 min, and 10 M at 120 and 240 min (lanes 3, 5, 8, and 9). D, results were analyzed and RUA illustrated, finding significant results at 1 M at 240 versus 0, 5 M at 120 versus 0, and 10 M at 120 versus 0 min.

     

     

  • Data from [The Journal of Biological Chemistry 2010.October;285:32824-32833]
    PD98059 purchased from Selleck


  • Click to enlarge

    We used real time RT-PCR to investigate the effects of PD98059 on SRP72 mRNA expression. All the samples were treated under the same experimental conditions used in protein tests done by WB, and phosphorylation was measured indirectly by IP-WB. The results did not show significant changes on the mRNA expression of SRP72 after the treatment with these inhibitors.

     

     

  • We used real time RT-PCR to investigate the effects of PD98059 on SRP72 mRNA expression. All the samples were treated under the same experimental conditions used in protein tests done by WB, and phosphorylation was measured indirectly by IP-WB. The results did not show significant changes on the mRNA expression of SRP72 after the treatment with these inhibitors.

     

     

  • Data from [The Journal of Biological Chemistry 2010.October;285:32824-32833]
    PD98059 purchased from Selleck

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T47D cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of  PD98059 for 24 hours.

 

 

Data independently produced by Dr. Zhang of Tianjin Medical University


effect of ERK1/2 inhibitor PD98059 (1, 5, and 10 M) on SRP72 protein expression was evaluated on Jurkat cells stimulated with rhIL-1. The cells were harvested at 0,120, and 240 min, and the protein expression was verified byWBusing antibodies against human SRP72, human SRP54 (nonphosphorylated SRP protein), and humanGAPDHas constitutive protein.Adecreased SRP72 expression at 10M and 240 min was found.

 

 

Data from [The Journal of Biological Chemistry 2010.October;285:32824-32833]

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