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662005 U0126 - CAS 109511-58-2 - Calbiochem

U0126, CAS 109511-58-2, is a 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.

U0126 - CAS 109511-58-2 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 1,4-Diamino-2,3-dicyano-1,4-bis(2-aminophenylthio)butadiene, MEK Inhibitor VI

Primary Target: MEK1 and MEK2
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662005
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
109511-58-2C₁₈H₁₆N₆S₂•½C₂H₅OH

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      662005-5MG
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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
          Quality LevelMQ100
          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
          Global Trade Item Number
          Catalogue Number GTIN
          662005-1MG 07790788052249
          662005-5MG 04055977261011

          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
          An Introduction to Inhibitors and Their Biological Applications - 1st Edition

          Data Sheet

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

          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 Protect from light
          -20°C
          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.
          		•