General 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.

Legal Information

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

Other Notes

Duncia, J.V., et al. 1998. Bioorg. Med. Chem. Lett.8, 2839.

Packaging

5 mg in Glass bottle

Packaged under inert gas

Physical form

A 100 mM (5 mg/124 µl) solution of U0126 (Cat. No. 662005) in DMSO.

Reconstitution

Following initial thaw, aliquot into precooled vials, freeze immediately at (-70°C).

Warning

Toxicity: Irritant (B)