MK-886

MK-886 (118414-82-7) is an inhibitor of leukotriene biosynthesis(IC50 = 2.5 nM in human PMN)1 via 5-lipoxygenase-activating protein (FLAP) inhibition (IC50 = 30 nM)2. MK-886 also inhibits PPARα (80% inhibition at 10 μM).3

White Solid

MK-886 is a potent and selective inhibitor of FLAP and Cox-1.

Binds to 5-lipoxygenase-activating protein with high affinity and prevents the activation of 5-lipoxygenase, thus inhibiting the biosynthesis of leukotrienes.

ChEBI: A member of the class of indoles that is 1H-indole substituted by a isopropyl group at position 5, a tert-butylsulfanediyl group at position 3, a 4-chlorobenzyl group at position 1 and a 2-carboxy-2-methylpropyl group at pos tion 2. It acts as an inhibitor of arachidonate 5-lipoxygenase.

An inhibitor of leukotriene biosynthesis (IC 50 = 3 nM in human polymorphonuclear leukocytes). Acts by inhibiting 5-lipoxygenase-activating protein (FLAP) (IC 50 = 30 nM for inhibition of [ 125 I]-L-691,678 photoaffinity labelling). Also moderately potent PPAR α antagonist (IC 50 = 0.5-1 μ M). Orally active in vivo .

Store at RT

[1] J GILLARD. L-663,536 (MK-886) (3-[1-(4-chlorobenzyl)-3-t-butyl-thio-5-isopropylindol-2-yl]-2,2 - dimethylpropanoic acid), a novel, orally active leukotriene biosynthesis inhibitor.[J]. Canadian journal of physiology and pharmacology, 1989, 67 5: 456-464. DOI:10.1139/y89-073
[2] J F EVANS. 5-Lipoxygenase-activating protein is the target of a quinoline class of leukotriene synthesis inhibitors.[J]. Molecular Pharmacology, 1991, 40 1: 22-27.
[3] JAMES P. KEHRER. Inhibition of peroxisome-proliferator-activated receptor (PPAR)alpha by MK886.[J]. The Ukrainian Biochemical Journal, 2001, 78 1: 899-906. DOI:10.1042/0264-6021:3560899