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

513000
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      Overview

      Key Spec Table

      Empirical Formula CAS #
      C₁₆H₁₃NO₃167869-21-8

      Pricing & Availability

      Catalogue NumberAvailability Packaging Qty/Pack Price Quantity
      513000-10MG
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          10 mg
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          513000-25MG
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              25 mg
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              513000-5MG
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                  5 mg
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                  Description
                  Overview Selective, 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 Number 513000
                  Brand Family Calbiochem®
                  Synonyms 2ʹ-Amino-3ʹ-methoxyflavone, MEK Inhibitor V
                  References
                  References 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.
                  Product Information
                  CAS number 167869-21-8
                  ATP Competitive N
                  Form Pale yellow solid
                  Hill Formula C₁₆H₁₃NO₃
                  Chemical formula C₁₆H₁₃NO₃
                  Molar Mass 267.3
                  Reversible Y
                  Structure formula Image
                  Applications
                  Biological Information
                  Primary Target MAP kinase kinase (MEK)
                  Primary Target IC50 2 µM against NGF-induced increase in MAP kinase activity
                  Purity ≥98% by HPLC
                  Physicochemical Information
                  Cell permeable Y
                  Solubility DMSO or MeOH
                  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 No
                  Special Instructions Following 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

                  Documentation

                  MSDS

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                  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.

                  Revision 21-January-2014 JSW
                  Synonyms 2ʹ-Amino-3ʹ-methoxyflavone, MEK Inhibitor V
                  Description Selective, 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.
                  Form Pale yellow solid
                  CAS number 167869-21-8
                  Molar mass 267.3
                  Chemical formula C₁₆H₁₃NO₃
                  Structure formula
                  Purity ≥98% by HPLC
                  Solubility DMSO (20 mg/ml) or Methanol (0.7 mg/ml)
                  Storage -20°C
                  Protect from light
                  Do Not Freeze No
                  Special Instructions Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 4 months at -20°C.
                  Toxicity Standard Handling
                  References 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.
                  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.