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.

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

Proprietà

• Livello qualitativo: 100
• Saggio: ≥95% (HPLC)
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; desiccated (hygroscopic); protect from light
• Colore: beige
• Solubilità: DMSO: 25 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: −20°C

Descrizione

Descrizione generale

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).

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Regulatory Review (Z)

Ricostituzione

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

Altre note

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

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable