662005 U0126 - CAS 109511-58-2 - Calbiochem

662005
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₈H₁₆N₆S₂•½C₂H₅OH 109511-58-2

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      662005-10MG
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          Plastic ampoule 10 mg
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          662005-1MG
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              Glass bottle 1 mg
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              662005-20MG
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                  Plastic ampoule 20 mg
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                  662005-5MG
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                      Glass bottle 5 mg
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                      Description
                      OverviewA potent and specific inhibitor of MEK1 (IC50 = 72 nM) and MEK2 (IC50 = 58 nM). The inhibition is noncompetitive with respect to both ATP and ERK. Has very little effect on other kinases such as Abl, Cdk2, Cdk4, ERK, JNK, MEKK, MKK-3, MKK-4/SEK, MKK-6, PKC, and Raf. Shown to block doxazosin-induced osteoblastic differentiation. Also acts as an immunosuppressant by effectively blocking IL-2 synthesis and T cell proliferation without affecting the long-term outcomes of either T cell activation or tolerance. Noncompetitive with respect to ATP. Also available in InSolution™ format (Cat. No. 662009).
                      Catalogue Number662005
                      Brand Family Calbiochem®
                      Synonyms1,4-Diamino-2,3-dicyano-1,4-bis(2-aminophenylthio)butadiene, MEK Inhibitor VI
                      References
                      ReferencesChoi, Y.J., et al. 2011. Biochem. Biophys. Res. Commun. 416, 232.
                      DeSilva, D.R., et al. 1998. J. Immunol. 160, 4175.
                      Duncia, J.V., et al. 1998. Biorg. Med. Chem. Lett. 8, 2839.
                      Favata, M.F., et al. 1998. J. Biol. Chem. 273, 18623.
                      Product Information
                      CAS number109511-58-2
                      ATP CompetitiveN
                      FormWhite solid
                      Hill FormulaC₁₈H₁₆N₆S₂•½C₂H₅OH
                      Chemical formulaC₁₈H₁₆N₆S₂•½C₂H₅OH
                      ReversibleN
                      Structure formula ImageStructure formula Image
                      Applications
                      Biological Information
                      Primary TargetMEK1 and MEK2
                      Primary Target IC<sub>50</sub>72 nM, 58 nm, against MEK1, and MEK2, respectively
                      Purity≥98% by HPLC
                      Physicochemical Information
                      Cell permeableN
                      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 InstructionsUnstable in solution; reconstitute just prior to use.
                      Packaging Information
                      Packaged under inert gas Packaged under inert gas
                      Transport Information
                      Supplemental Information
                      Specifications

                      Documentation

                      U0126 - CAS 109511-58-2 - Calbiochem SDS

                      Title

                      Safety Data Sheet (SDS) 

                      U0126 - CAS 109511-58-2 - Calbiochem Certificates of Analysis

                      TitleLot Number
                      662005

                      References

                      Reference overview
                      Choi, Y.J., et al. 2011. Biochem. Biophys. Res. Commun. 416, 232.
                      DeSilva, D.R., et al. 1998. J. Immunol. 160, 4175.
                      Duncia, J.V., et al. 1998. Biorg. Med. Chem. Lett. 8, 2839.
                      Favata, M.F., et al. 1998. J. Biol. Chem. 273, 18623.

                      Brochure

                      Title
                      MAPK Pathway Poster ( 750 KB )

                      Citations

                      Title
                    • Choi, Y.J., et al. 2011. Biochem. Biophys. Res. Commun. 416, 232.
                    • Oliveira, J.B., et al. 2007. Procedings of the National Academy of Science 104, 8953.
                    • Chengyu Wu and Jiaoti Huang. 2007. Journal of Biological Chemistry 282, 3571.
                    • 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,.
                    • Thiel, A., et al. 2006. Journal of Biological Chemistry 281, 4564.
                    • Basak, C., et al. 2005. Journal of Immunology 174, 5672.
                    • Soonkyu Chung, et al. (2005) Conjugated linoleic acid promotes human adipocyte insulin resistance through NF-κB-dependent cytokine production. Journal of Biological Chemistry 280, 38445-38456.
                    • Marie-Claire Delfini, et al. (2005) Control of the segmentation process by graded MAPK/ERK activation in the chick embryo. Proceedings of the National Academy of Science USA 102, 11343-11348.
                    • Gutzmer, R., et al. 2005. Journal of Immunology 5224.
                    • Monick, M.M., et al. 2005. Journal of Biological Chemistry 280, 2147.
                    • Tang, Q-Q., et al. 2005. Proceedings of the National Academy of Sciences (USA) 102, 9766.
                    • Junji Tsurutani, et al. (2005) Inhibition of the phosphatidylinositol 3-kinase/Akt/Mammalian target of rapamycin pathway but no the MEK/ERK Pathway attentuates laminin-meidated small cell lunch cancer cellular survival and resistance to Imatinib mesylate or chemolyte.. Cancer Research 65, 8423-8432.
                    • Wojciechowski, W., et al. 2005. Journal of Immunology 174, 7859.
                    • Wu, M-H., et al. 2005. The Journal of Clinical Endocrinology & Metabolism 90, 286.
                    • 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.
                    • Naoto Inukai, et al. (2004) A novel hydrogen peroxide-induced phosphorylation and ubiquitination pathway leading to RNA polymerase II proteolysis. Journal of Biological Chemistry 279, 8190-8195.
                    • 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.
                    • 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.
                    • 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.

                      Revision28-February-2012 RFH
                      Synonyms1,4-Diamino-2,3-dicyano-1,4-bis(2-aminophenylthio)butadiene, MEK Inhibitor VI
                      DescriptionA potent and specific inhibitor of MEK1 (IC50 = 72 nM) and MEK2 (IC50 = 58 nM). The inhibition is noncompetitive with respect to MEK substrates, ATP and ERK. Has very little effect on other kinases, such as Abl, Cdk2, Cdk4, ERK, JNK, MEKK, MKK-3, MKK-4/SEK, MKK-6, PKC, and Raf. Shown to block doxazosin-induced osteoblastic differentiation. U0126 also acts as an immunosuppressant by effectively blocking IL-2 synthesis and T cell proliferation without affecting the long-term outcomes of either T cell activation or tolerance. Noncompetitive with respect to ATP. Also available in InSolution™ format (Cat. No. 662009.
                      FormWhite solid
                      Intert gas (Yes/No) Packaged under inert gas
                      CAS number109511-58-2
                      Chemical formulaC₁₈H₁₆N₆S₂•½C₂H₅OH
                      Structure formulaStructure formula
                      Purity≥98% by HPLC
                      SolubilityDMSO (200 mg/ml)
                      Storage -20°C
                      Protect from light
                      Do Not Freeze Ok to freeze
                      Special InstructionsUnstable in solution; reconstitute just prior to use.
                      Toxicity Standard Handling
                      ReferencesChoi, Y.J., et al. 2011. Biochem. Biophys. Res. Commun. 416, 232.
                      DeSilva, D.R., et al. 1998. J. Immunol. 160, 4175.
                      Duncia, J.V., et al. 1998. Biorg. Med. Chem. Lett. 8, 2839.
                      Favata, M.F., et al. 1998. J. Biol. Chem. 273, 18623.
                      Citation
                    • Choi, Y.J., et al. 2011. Biochem. Biophys. Res. Commun. 416, 232.
                    • Oliveira, J.B., et al. 2007. Procedings of the National Academy of Science 104, 8953.
                    • Chengyu Wu and Jiaoti Huang. 2007. Journal of Biological Chemistry 282, 3571.
                    • 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,.
                    • Thiel, A., et al. 2006. Journal of Biological Chemistry 281, 4564.
                    • Basak, C., et al. 2005. Journal of Immunology 174, 5672.
                    • Soonkyu Chung, et al. (2005) Conjugated linoleic acid promotes human adipocyte insulin resistance through NF-κB-dependent cytokine production. Journal of Biological Chemistry 280, 38445-38456.
                    • Marie-Claire Delfini, et al. (2005) Control of the segmentation process by graded MAPK/ERK activation in the chick embryo. Proceedings of the National Academy of Science USA 102, 11343-11348.
                    • Gutzmer, R., et al. 2005. Journal of Immunology 5224.
                    • Monick, M.M., et al. 2005. Journal of Biological Chemistry 280, 2147.
                    • Tang, Q-Q., et al. 2005. Proceedings of the National Academy of Sciences (USA) 102, 9766.
                    • Junji Tsurutani, et al. (2005) Inhibition of the phosphatidylinositol 3-kinase/Akt/Mammalian target of rapamycin pathway but no the MEK/ERK Pathway attentuates laminin-meidated small cell lunch cancer cellular survival and resistance to Imatinib mesylate or chemolyte.. Cancer Research 65, 8423-8432.
                    • Wojciechowski, W., et al. 2005. Journal of Immunology 174, 7859.
                    • Wu, M-H., et al. 2005. The Journal of Clinical Endocrinology & Metabolism 90, 286.
                    • 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.
                    • Naoto Inukai, et al. (2004) A novel hydrogen peroxide-induced phosphorylation and ubiquitination pathway leading to RNA polymerase II proteolysis. Journal of Biological Chemistry 279, 8190-8195.
                    • 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.
                    • 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.