MEK Inhibitor VII - CAS 305350-87-2 - Calbiochem

A cell-permeable vinylogous cyanamide that acts as a selective inhibitor of MEK1/2 (IC₅₀ = 180 nM and 220 nM, respectively). Shown to inhibit AP-1 activity (IC₅₀ = 2.03 µM). Inhibits ERK1, MKK3/p38, MKK4, JNK, and PKC activities at higher concentrations (IC₅₀ >10 µM). Reported to offer neuroprotection against ischemic brain injury in mice by selectively blocking ERK1/2 activation. Also suppresses IL-1β expression. Displays enhanced aqueous solubility compared to U0126 (Cat. No. 662005). Uncompetitive with respect to ATP.

A cell-permeable, vinylogous cyanamide that acts as a selective inhibitor of MEK1 (IC₅₀ = 180 nM) and MEK2 (IC₅₀ = 220 nM). Also shown to inhibit AP-1 activity (IC₅₀ = 2.03 µM). Inhibits ERK1, MKK3/p38, MKK4, JNK, and PKC activities only at higher concentrations (IC₅₀ >10 µM). Reported to exhibit neuroprotective effects against ischemic brain injury in mice by selectively blocking ERK1/2 activation (i.e. noncompetitive with respect to ATP). Also reported to suppress IL-1β expression. Displays enhanced aqueous solubility compared to U0126 (Cat. No. 662005). Supplied as a mixture of Z- and E-isomers.

Supplied as a mixture of Z- and E-isomers.

Cell permeable: yes

Primary Target
MEK 1, MEK 2

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 180 nM and 220 nM against MEK1 and MEK2, respectively

Packaged under inert gas

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Hetman, M., et al. 2002. J. Biol. Chem.277, 49577.
Ohno, M., et al. 2001. Nat. Neurosci.4, 1238.
Wang, H., et al. 2001. Biochem. Biophys. Res. Commun.286, 869.
Scherle, P.A., et al. 2000. J. Biol. Chem.275, 37086.
Valjent, E., et al. 2000. J. Neurosci.20, 8701.
Watabe, A.M., et al. 2000. J. Neurosci.20, 5924.
Atkins, C.M., et al. 1998. Nat. Neurosci.1, 602.

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

Toxicity: Standard Handling (A)