MK-886 - CAS 118414-82-7 - Calbiochem

General description

A cell-permeable, orally active NSAID (nonsteroidal antiinflammatory drug) that blocks cellular Cox pathway PGE2 (prostaglandin E₂) production by inhibiting COX-1 and mPGES-1 (microsomal PGE₂ synthase-1), but not COX-2, activity (IC₅₀ = 8, 2, and 58 M, respectively), as well as suppresses cellular 5-LO (5-Lypoxygenase; Cat. No. 437996) pathway activation by inhibiting FLAP (5-LO-activating protein), rather than 5-LO, activity (<10% by 1 M MK-886). Unlike NSAIDs (nonsteroidal antiinflammatory drugs) that target only COX pathway, MK-886 does not cause gastrointestinal damages when applied in vivo.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
leukotreine biosybthesis

Product does not compete with ATP.

Reversible: no

Warning

Toxicity: Standard Handling (A)

Other Notes

Koeberle, A., et al. 2009. Eur. J. Pharmacol.608, 84.
Koeberle, A., et al. 2008. J. Pharmacol. Exp. Ther.326, 975.
Fisher, L., et al. 2007. Br. J. Pharmacol.152, 471.
Ford-Hutchinson, A.W., et al. 1993. Can. J. Physiol. Pharmacol. 71, 806.
Ford-Hutchinson, A.W. 1991. Trends Pharmacol.12, 68.
Dixon, R.A., et al. 1990. Nature 343, 282.
Rouzer, C.A., et al. 1990. J. Biol. Chem.265, 1436.

Legal Information

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