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513000 PD 98059 - CAS 167869-21-8 - Calbiochem

PD 98059, CAS 167869-21-8, is a cell-permeable, selective & reversible inhibitor of MAP Kinase Kinase (MEK). Inhibits MAP Kinase activation and subsequent phosphorylation of MAP Kinase substrates.

PD 98059 - CAS 167869-21-8 - Calbiochem: Ficha de dados de segurança do material (FDSM) ou ficha de segurança do material (FSM), certificado de análise (CA) e certificado de qualidade (CQ), dossiês e outros documentos disponíveis.

Sinônimos: 2ʹ-Amino-3ʹ-methoxyflavone, MEK Inhibitor V

Primary Target: MAP kinase kinase (MEK)
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CAS #Empirical Formula
167869-21-8C₁₆H₁₃NO₃

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      Description
      OverviewSelective, reversible, and cell-permeable inhibitor of MAP kinase kinase (MEK) that acts by inhibiting the activation of MAP kinase and subsequent phosphorylation of MAP kinase substrates. Pretreatment of PC-12 cells with PD 98059 completely blocks the 4-fold increase in MAP kinase activity produced by nerve growth factor (NGF; IC50 = 2 µM); however, it has no effect on NGF-dependent tyrosine phosphorylation of the p140trk receptor or its substrate Shc and does not block NGF-dependent activation of PI 3-kinase. Blocks LPS-induced activation of TNF-α gene expression. Inhibits cell growth and reverses the phenotype of ras-transformed BALB3T3 mouse fibroblasts and rat kidney cells. A 5 mg/ml solution of PD 98059 (Cat. No. 513001) in anhydrous DMSO is also available.
      Catalogue Number513000
      Brand Family Calbiochem®
      Synonyms2ʹ-Amino-3ʹ-methoxyflavone, MEK Inhibitor V
      References
      ReferencesMeans, T.K., et al. 2000. J. Leukoc. Biol. 67, 885.
      Kültz, D., et al. 1998. J. Biol. Chem. 273, 13645.
      Dudley, D.T., et al. 1995. Proc. Natl. Acad. Sci. USA 92, 7686.
      Langlois, W.J., et al. 1995. J. Biol. Chem. 270, 25320.
      Pang, L., et al. 1995. J. Biol. Chem. 270, 13585.
      Waters, S.B., et al. 1995. J. Biol. Chem. 270, 20883.
      Product Information
      CAS number167869-21-8
      ATP CompetitiveN
      FormPale yellow solid
      Hill FormulaC₁₆H₁₃NO₃
      Chemical formulaC₁₆H₁₃NO₃
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetMAP kinase kinase (MEK)
      Primary Target IC<sub>50</sub>2 µM against NGF-induced increase in MAP kinase activity
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 4 months at -20°C.
      Packaging Information
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Número de catálogo GTIN
      513000-5MG 07790788050917

      Documentation

      PD 98059 - CAS 167869-21-8 - Calbiochem MSDS

      Título

      Ficha de Segurança de Produtos (MSDS) 

      PD 98059 - CAS 167869-21-8 - Calbiochem Certificados de análise

      TítuloNúmero do lote
      513000

      Referências

      Visão geral de referência
      Means, T.K., et al. 2000. J. Leukoc. Biol. 67, 885.
      Kültz, D., et al. 1998. J. Biol. Chem. 273, 13645.
      Dudley, D.T., et al. 1995. Proc. Natl. Acad. Sci. USA 92, 7686.
      Langlois, W.J., et al. 1995. J. Biol. Chem. 270, 25320.
      Pang, L., et al. 1995. J. Biol. Chem. 270, 13585.
      Waters, S.B., et al. 1995. J. Biol. Chem. 270, 20883.

      Ficha de dados

      Título
      Reprogramming Cell Fate and Function Novel Strategies for iPSC Generation, Characterization, and Differentiation

      Pôster

      Título
      Human Kinome & InhibitorSelect™ Libraries

      Citações

      Título
    • Joao B. Oliveira, et al. (2007) NRAS mutation causes a human autoimmune lymphoproliferative syndrome. Procedings of the National Academy of Science 104, 8953-8958.
    • Alexandra Thiel, Mira Heinonen, Johanna Rintahaka, Tuija Hallikainen, and Annabrita Hemmes, Dan A. Dixon, Caj Haglund, and Ari Ristimaki. (2006) EXPRESSION OF CYCLOOXYGENASE-2 IS REGULATED BY GSK-3 IN GASTRIC CANCER CELLS. Journal of Biological Chemistry in press,.
    • Farahdiba Jafri, et al. (2006) Constitutive ERK1/2 activation by a chimeric neurokinin NK1 receptor-beta-arrestin1 fusion protein: Probing the composition and function of the G protein-coupled receptor 'signalsome'. Journal of Biological Chemistry in press,.
    • Alexandra Thiel, et al. (2006) Expression of Cyclooxygenase-2 Is Regulated by Glycogen Synthase Kinase-3beta in Gastric Cancer Cells. Journal of Biological Chemistry 281, 4564-4569.
    • Bysani Chandrasekar, et al. (2005) The pro-atherogenic cytokine interleukin-18 induces CXCL16 expression in rat aortic smooth muscle cells via MyD88, interleukin-1 receptor-associated kinase, tumor necrosis factor receptor-associated factor 6, c-Src, phosphatidylinositol 3-kinase, Akt, c-J. Journal of Biological Chemistry 280, 26263-26277.
    • Diane Gesty-Palmer, et al. (2005) b-Arrestin 2 expression determines the transcriptional response to lysophosphatidic acid stimulation in murine embryo fibroblasts. Journal of Biological Chemistry 280, 32157-32167.
    • Renee M. Marshall, et al. (2005) Cyclin T1 expression is regulated by multiple signaling pathways and mechanisms during activation of human peripheral blood lymphocytes. Journal of Immunology 175, 6402-6411.
    • Wojciech Wojciechowski, et al. (2005) Enhanced Expression of CD20 in Human Tumor B Cells is Controlled Through ERK-Dependent Mechanisms. Journal of Immunology 174, 7859-7868.
    • Yung-Luen Yu, et al. (2005) MAP kinase-mediated phosphorylation of GATA-1 promotes Bcl-XL expression and cell survival. Journal of Biological Chemistry 280, 29533-29542.
    • Yona Goldshmit, et al. (2004) SOCS2 Induces Neurite Outgrowth by Regulation of Epidermal Growth Factor Receptor Activation. Journal of Biological Chemistry 279, 16349-16355.
    • Rick B. Vega, et al. (2004) Protein Kinases C and D Mediate Agonist-Dependent Cardiac Hypertrophy through Nuclear Export of Histone Deacetylase 5. Molecular and Cellular Biology 24, 8374-8385.
    • Xinbo Liao, et al. (2003) Androgen stimulates matrix metalloproteinase-2 expression in human prostate cancer. Endocrinology 144, 1656-1663.
    • Michael J. Cross, et al. (2002) The Shb Adaptor Protein Binds to Tyrosine 766 in the FGFR-1 and Regulates the Ras/MEK/MAPK Pathway via FRS2 Phosphorylation in Endothelial Cells. Molecular Biology of the Cell 13, 2881-2893.
    • Maryse Delehedde, et al. (2002) Fibroblast growth factor-2 binds to small heparin-derived oligosaccharides and stimulates a sustained phosphorylation of p42/44 mitogen-activated protein kinase and proliferation of rat mammary fibroblasts. Biochemistry Journal 366, 235-244.
    • Silja Wessler, et al. (2000) Helicobacter pylori activates the histidine decarboxylase promoter through a mitogen-activated protein kinase pathway independent of pathogenicity island-encoded virulence factors. Journal of Biological Chemistry 275, 3629-3636.
      		•
      Ficha de dados

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision21-January-2014 JSW
      Synonyms2ʹ-Amino-3ʹ-methoxyflavone, MEK Inhibitor V
      DescriptionSelective, reversible, and cell-permeable inhibitor of MAP kinase kinase (MEK) that acts by inhibiting the activation of MAP kinase and subsequent phosphorylation of MAP kinase substrates (noncompetitive with respect to ATP). Pretreatment of PC-12 cells with PD 98059 completely blocks the 4-fold increase of MAP kinase activity produced by nerve growth factor (NGF; IC50 = 2 µM); however, it has no effect on NGF-dependent tyrosine phosphorylation of the pp140trk receptor or its substrate Shc and does not block NGF-dependent activation of PI 3-kinase. Inhibits cell growth and reverses the phenotype of ras-transformed BALB 3T3 mouse fibroblasts and rat kidney cells.
      FormPale yellow solid
      CAS number167869-21-8
      Chemical formulaC₁₆H₁₃NO₃
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (20 mg/ml) or Methanol (0.7 mg/ml)
      Storage Protect from light
      -20°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 4 months at -20°C.
      Toxicity Standard Handling
      ReferencesMeans, T.K., et al. 2000. J. Leukoc. Biol. 67, 885.
      Kültz, D., et al. 1998. J. Biol. Chem. 273, 13645.
      Dudley, D.T., et al. 1995. Proc. Natl. Acad. Sci. USA 92, 7686.
      Langlois, W.J., et al. 1995. J. Biol. Chem. 270, 25320.
      Pang, L., et al. 1995. J. Biol. Chem. 270, 13585.
      Waters, S.B., et al. 1995. J. Biol. Chem. 270, 20883.
      Citation
    • Joao B. Oliveira, et al. (2007) NRAS mutation causes a human autoimmune lymphoproliferative syndrome. Procedings of the National Academy of Science 104, 8953-8958.
    • Alexandra Thiel, Mira Heinonen, Johanna Rintahaka, Tuija Hallikainen, and Annabrita Hemmes, Dan A. Dixon, Caj Haglund, and Ari Ristimaki. (2006) EXPRESSION OF CYCLOOXYGENASE-2 IS REGULATED BY GSK-3 IN GASTRIC CANCER CELLS. Journal of Biological Chemistry in press,.
    • Farahdiba Jafri, et al. (2006) Constitutive ERK1/2 activation by a chimeric neurokinin NK1 receptor-beta-arrestin1 fusion protein: Probing the composition and function of the G protein-coupled receptor 'signalsome'. Journal of Biological Chemistry in press,.
    • Alexandra Thiel, et al. (2006) Expression of Cyclooxygenase-2 Is Regulated by Glycogen Synthase Kinase-3beta in Gastric Cancer Cells. Journal of Biological Chemistry 281, 4564-4569.
    • Bysani Chandrasekar, et al. (2005) The pro-atherogenic cytokine interleukin-18 induces CXCL16 expression in rat aortic smooth muscle cells via MyD88, interleukin-1 receptor-associated kinase, tumor necrosis factor receptor-associated factor 6, c-Src, phosphatidylinositol 3-kinase, Akt, c-J. Journal of Biological Chemistry 280, 26263-26277.
    • Diane Gesty-Palmer, et al. (2005) b-Arrestin 2 expression determines the transcriptional response to lysophosphatidic acid stimulation in murine embryo fibroblasts. Journal of Biological Chemistry 280, 32157-32167.
    • Renee M. Marshall, et al. (2005) Cyclin T1 expression is regulated by multiple signaling pathways and mechanisms during activation of human peripheral blood lymphocytes. Journal of Immunology 175, 6402-6411.
    • Wojciech Wojciechowski, et al. (2005) Enhanced Expression of CD20 in Human Tumor B Cells is Controlled Through ERK-Dependent Mechanisms. Journal of Immunology 174, 7859-7868.
    • Yung-Luen Yu, et al. (2005) MAP kinase-mediated phosphorylation of GATA-1 promotes Bcl-XL expression and cell survival. Journal of Biological Chemistry 280, 29533-29542.
    • Yona Goldshmit, et al. (2004) SOCS2 Induces Neurite Outgrowth by Regulation of Epidermal Growth Factor Receptor Activation. Journal of Biological Chemistry 279, 16349-16355.
    • Rick B. Vega, et al. (2004) Protein Kinases C and D Mediate Agonist-Dependent Cardiac Hypertrophy through Nuclear Export of Histone Deacetylase 5. Molecular and Cellular Biology 24, 8374-8385.
    • Xinbo Liao, et al. (2003) Androgen stimulates matrix metalloproteinase-2 expression in human prostate cancer. Endocrinology 144, 1656-1663.
    • Michael J. Cross, et al. (2002) The Shb Adaptor Protein Binds to Tyrosine 766 in the FGFR-1 and Regulates the Ras/MEK/MAPK Pathway via FRS2 Phosphorylation in Endothelial Cells. Molecular Biology of the Cell 13, 2881-2893.
    • Maryse Delehedde, et al. (2002) Fibroblast growth factor-2 binds to small heparin-derived oligosaccharides and stimulates a sustained phosphorylation of p42/44 mitogen-activated protein kinase and proliferation of rat mammary fibroblasts. Biochemistry Journal 366, 235-244.
    • Silja Wessler, et al. (2000) Helicobacter pylori activates the histidine decarboxylase promoter through a mitogen-activated protein kinase pathway independent of pathogenicity island-encoded virulence factors. Journal of Biological Chemistry 275, 3629-3636.
      		•