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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. 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. 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. Reported to undergo rapid isomerization in DMSO and exist as an equilibrium mixture of (Z,Z), E,E) and (Z,E) isomers with minimal loss of activity over a period of 1 month.
Catalogue Number
662009
Brand Family
Calbiochem®
References
References
Duncia, J.V., et al. 1998. Bioorg. Med. Chem. Lett.8, 2839.
Product Information
CAS number
109511-58-2
Form
Liquid
Formulation
A 100 mM (5 mg/124 µl) solution of U0126 (Cat. No. 662005) in DMSO.
InSolution™ U0126 - CAS 109511-58-2 - Calbiochem 分析证书
标题
批号
662009
参考
参考信息概述
Duncia, J.V., et al. 1998. Bioorg. Med. Chem. Lett.8, 2839.
数据表
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.
Revision
09-January-2012 RFH
Description
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. 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. 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. Reported to undergo rapid isomerization in DMSO and exist as an equilibrium mixture of (Z,Z), E,E) and (Z,E) isomers with minimal loss of activity over a period of 1 month.
Form
Liquid
Formulation
A 100 mM (5 mg/124 µl) solution of U0126 (Cat. No. 662005) in DMSO.
Intert gas (Yes/No)
Packaged under inert gas
CAS number
109511-58-2
Chemical formula
C₁₈H₁₆N₆S₂•½C₂H₅OH
Structure formula
Purity
≥98% by HPLC
Storage
Protect from light
Avoid freeze/thaw
≤ -70°C
Hygroscopic
Do Not Freeze
Ok to freeze
Special Instructions
Following initial thaw, aliquot into precooled vials, freeze immediately at (-70°C).
Toxicity
Irritant
References
Duncia, J.V., et al. 1998. Bioorg. Med. Chem. Lett.8, 2839.
