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.

• Synonim(y): MEK Inhibitor I
• Wzór empiryczny (zapis Hilla): C₂₁H₁₈N₄OS
• Numer CAS: 297744-42-4
• Masa cząsteczkowa: 374.46
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Poziom jakości: 100
• Próba: ≥95% (sum of two isomers, HPLC)
• Formularz: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: white
• rozpuszczalność: DMSO: 10 mg/mL; methanol: 50 mg/mL
• Warunki transportu: wet ice
• temp. przechowywania: −20°C

Opis

Opis ogólny

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.).

Działania biochem./fizjol.

Cell permeable: yes

Primary Target
MEK

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 12 nM against MEK

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Rekonstytucja

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

Inne uwagi

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

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 1
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable