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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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      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

      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.
      		•