Biochem/physiol Actions

Cell permeable: no

Reversible: no

Target IC₅₀: 72 nM, 58 nm, against MEK1, and MEK2, respectively

Primary TargetMEK1 and MEK2

Product does not compete with ATP.

General description

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).

Legal Information

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

Other Notes

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.

Packaging

1, 5 mg in Glass bottle

Packaged under inert gas

10, 20 mg in Plastic ampoule

Reconstitution

Unstable in solution; reconstitute just prior to use.

Warning

Toxicity: Standard Handling (A)