U0126 - CAS 109511-58-2 - Calbiochem (C15-1203-491)

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).

Biochem/physiol Actions

Cell permeable: no

Primary Target
MEK1 and MEK2

Product does not compete with ATP.

Reversible: no

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

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Unstable in solution; reconstitute just prior to use.

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.

Legal Information

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