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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 MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

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

Primary Target: MAP kinase kinase (MEK)
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513000
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
167869-21-8C₁₆H₁₃NO₃

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      513000-25MG
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          513000-5MG
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              		 Glass bottle 5 mg
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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
              Catalogue Number GTIN
              513000-10MG 04055977272109
              513000-25MG 04055977272116
              513000-5MG 07790788050917

              Documentation

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

              Title

              Safety Data Sheet (SDS) 

              PD 98059 - CAS 167869-21-8 - Calbiochem Certificates of Analysis

              TitleLot Number
              513000

              References

              Reference overview
              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.

              Citations

              Title
            • 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.
              		•
              Data Sheet

              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.
              		•