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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
              662005-10MGCN 04055977261691
              662005-1MGCN 07790788052249
              662005-5MGCN 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.
              		•