475964

MK-2 Inhibitor IV, MK-25

The MK-2 Inhibitor IV, MK-25 controls the biological activity of MK-2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Sinônimo(s): 5-(4-Chlorophenyl)-N-(4-(piperazin-1-yl)phenyl)-N-(pyridin-2-ylmethyl)furan-2-carboxamide, HCl, MAPKAP-K2 Inhibitor IV, MK-25
• Código UNSPSC: 12352200
• NACRES: NA.28

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥95% (HPLC)
• Formulário: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; desiccated (hygroscopic); protect from light
• cor: beige
• solubilidade: DMSO: 25 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: −20°C

Descrição

Descrição geral

A cell-permeable furanylcarboxamide compound that acts as a potent, reversible and non-ATP-competitive inhibitor of MK-2/MAPKAP-K2 activity (IC₅₀ = 110 nM; EC₅₀ = 350 nM for pHSP27 in IL-1β-stimulated SW1353 cells) with excellent selectivity over 150 kinases (% activity inhibition at 10 µM against human CK2, Haspin, Arg and CK1γ3 = 40, 40, 42 and >70, respectively). Shown to efficiently suppress the secretions of TNFα, IL6 (IC₅₀ = 4.4 and 5.2 µM in LPS-stimulated THP1 cell, respectively) and MMP-13 (IC₅₀ = 5.7 and 2.2 µM in IL1β-stimulated SW1353 and in primary osteoarthritis-derived chondrocytes, respectively). Exhibits desirable bioavailability and weakly inhibits a panel of cytochrome P450 isozymes (IC₅₀ >20 µM for 3A4, 2D6 and 2C9).

Embalagem

Packaged under inert gas

Advertência

Toxicity: Regulatory Review (Z)

Reconstituição

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Outras notas

Huang, X., et al. 2011. ACS Med. Chem. Lett.2, 632.

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 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable