MEK Inhibitor I

A cell-permeable pyridine-containing vinylogous cyanamide compound that acts as a potent and selective inhibitor of MEK (IC₅₀ = 12 nM) with little activity towards MKK3 and MKK4 (IC₅₀ >1 µM). The inhibition is noncompetitive with respect to ERK and the compound displays significant affinity only towards ATP-bound MEK (i.e. noncompetitive with respect to ATP). Exhibits superior potency, solubility, and stability compared to U0126 (Cat. No. 662005) in aqueous solutions. Shown to protect against phorbol ester-mediated ear edema in mice (ED₅₀ of 5 mg/kg, ip.).

A cell-permeable, potent, and selective inhibitor of MEK (IC₅₀ = 12 nM) with little activity towards MKK3 and MKK4 (IC₅₀ >1 µM). The inhibition is non-competitive with respect to ERK and the compound displays significant affinity only towards ATP-bound MEK (i.e. non-competitive with respect to ATP). Exhibits superior potency, solubility, and stability compared to U0126 (Cat. No. 662005) in aqueous solutions. Shown to protect against phorbol ester-mediated ear edema in mice (ED₅₀ of 5 mg/kg, ip.).

Cell permeable: yes

Primary Target
MEK

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 12 nM against MEK

Packaged under inert gas

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Wityak, J., et al. 2004. Bioorg. Med. Chem. Lett.14, 1483.

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