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.

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

Propiedades

• Nivel de calidad: 100
• Análisis: ≥95% (sum of two isomers, HPLC)
• formulario: solid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: white
• solubilidad: DMSO: 10 mg/mL; methanol: 50 mg/mL
• Condiciones de envío: wet ice
• temp. de almacenamiento: −20°C

Descripción

Descripción general

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.).

Acciones bioquímicas o fisiológicas

Cell permeable: yes

Primary Target
MEK

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 12 nM against MEK

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

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

Otras notas

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

Información legal

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

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 1
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable