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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
662005
Purchase on Sigma-Aldrich

Přehled

Replacement Information

Tabulka spec. kláve

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

Products

Katalogové čísloBalení ks/bal.
662005-10MG Plastová ampulka 10 mg
662005-1MG Skleněná láhev 1 mg
662005-20MG Plastová ampulka 20 mg
662005-5MG Skleněná láhev 5 mg
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
Katalogové číslo GTIN
662005-10MG 04055977261691
662005-1MG 07790788052249
662005-20MG 04055977261004
662005-5MG 04055977261011

Documentation

U0126 - CAS 109511-58-2 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

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

TitleLot Number
662005

References

Přehled odkazů
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

Název
  • 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.
    		•