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MK-886
- Development stage
- Preclinical
- Lead developer
- Merck
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
MK-886 is an experimental small molecule inhibitor primarily known for its potent inhibition of the 5-lipoxygenase activating protein (FLAP), a key regulator in leukotriene biosynthesis. By blocking FLAP, MK-886 suppresses the activity of 5-lipoxygenase (5-LOX), thereby reducing leukotriene production, which plays a significant role in inflammatory responses such as asthma and arthritis. Additionally, MK-886 acts as a moderate antagonist of peroxisome proliferator–activated receptor alpha (PPARα) and can induce apoptosis. It also exhibits inhibitory effects on cyclooxygenase 1 (COX‑1) and microsomal prostaglandin E synthase‑1 (mPGES‑1), but not COX‑2, further modulating eicosanoid pathways involved in inflammation[2][4][6][7][8]. The compound is orally active and has been used extensively as a research tool to study inflammation, allergy, cancer, cardiovascular disease, and related conditions.
- Other names
- CGS-81585CGS81585CGS 81585
02
Targets
PPARA (Peroxisome proliferator-activated receptor alpha)PGHS-1 (Prostaglandin G/H Synthase 1)PTGES (Microsomal prostaglandin E synthase-1)FLAP (Arachidonate 5-lipoxygenase-activating protein)MAPT (Microtubule-associated protein tau)
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