U0126-CAS 109511-58-2-Calbiochem

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一般描述

A 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.
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. 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).

包装

1, 5 mg in Glass bottle
10, 20 mg in Plastic ampoule
Packaged under inert gas

生化/生理作用

Primary Target
MEK1 and MEK2
Product does not compete with ATP.
Target IC₅₀: 72 nM, 58 nm, against MEK1, and MEK2, respectively
Reversible: no
Cell permeable: no

警告

Toxicity: Standard Handling (A)

重悬

Unstable in solution; reconstitute just prior to use.

其他说明

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.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

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