MK-2 Inhibitor IV, MK-25

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).

Packaged under inert gas

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

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

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

Toxicity: Regulatory Review (Z)