444937

MEK Inhibitor I

The MEK Inhibitor I, also referenced under CAS 297744-42-4, controls the biological activity of MEK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Sinônimo(s): MEK Inhibitor I
• Fórmula empírica (Notação de Hill): C₂₁H₁₈N₄OS
• Número CAS: 297744-42-4
• Peso molecular: 374.46
• Número MDL: MFCD00048369
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥95% (sum of two isomers, HPLC)
• Formulário: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: white
• solubilidade: DMSO: 10 mg/mL; methanol: 50 mg/mL
• Condições de expedição: wet ice
• temperatura de armazenamento: −20°C

Descrição

Descrição geral

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.).

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
MEK

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 12 nM against MEK

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Reconstituição

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

Outras notas

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

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 1
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable