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Beschreibung

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-1beta-stimulated SW1353 cells) with excellent selectivity over 150 kinases (% activity inhibition at 10 µ,M against human CK2, Haspin, Arg and CK1gamma3 = 40, 40, 42 and >70, respectively). Shown to efficiently suppress the secretions of TNFalpha, IL6 (IC50 = 4.4 and 5.2 µ,M in LPS-stimulated THP1 cell, respectively) and MMP-13 (IC50 = 5.7 and 2.2 µ,M in IL1beta-stimulated SW1353 and in primary osteoarthritis-derived chondrocytes, respectively). Exhibits desirable bioavailability and weakly inhibits a panel of cytochrome P450 isozymes (IC50 >20 µ,M for 3A4, 2D6 and 2C9).