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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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      662005-1MG
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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
                  662005-10MG 04055977261691
                  662005-1MG 07790788052249
                  662005-20MG 04055977261004
                  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.
                  		•