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Catalog No. T6893   CAS 118414-82-7
Synonyms: MK886, L 663536, MK 886

MK-886 is an inhibitor of leukotriene biosynthesis, inhibiting 5-lipoxygenase-activating protein (FLAP). It is also a moderately potent PPARα antagonist.

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MK-886, CAS 118414-82-7
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Purity: 98%
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Biological Description
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Description MK-886 is an inhibitor of leukotriene biosynthesis, inhibiting 5-lipoxygenase-activating protein (FLAP). It is also a moderately potent PPARα antagonist.
Targets&IC50 COX-2:58 μM, COX-1:8 μM
In vitro MK-886, an inhibitor of the 5-lipoxygenase-activating protein (FLAP), potently suppresses leukotriene biosynthesis in intact cells and is frequently used to define a role of the 5-lipoxygenase (EC pathway in cellular or animal models of inflammation, allergy, cancer, and cardiovascular disease. MK-886 inhibits isolated COX-1 (IC50=8 μM) and blocks the formation of the COX-1-derived products 12(S)-hydroxy-5-cis-8,10-trans-heptadecatrienoic acid (12-HHT) and thromboxane B2 in washed human platelets in response to collagen as well as from exogenous arachidonic acid (IC50=13–15 μM).Isolated COX-2 was less affected (IC50=58 μM), and in A549 cells, MK-886 (33 μM) failed to suppress COX-2-dependent 6-ketoprostaglandin (PG)F1α formation. MK-886 (10 μM) inhibits COX-1-mediated platelet aggregation induced by collagen or arachidonic acid whereas thrombin- or U-46619-induced (COX-independent) aggregation is not affected[1].
In vivo Repeated daily i.p. injections of MK-886 results in increased GluR1 phosphorylation in brain samples obtained from the prefrontal cortex. In contrast, a single injection of MK-886 does not alter cortical GluR1 phosphorylation[2].
Kinase Assay Enzyme assay is conducted in buffer containing 25 mM Tris, pH 8.0, 1 mM DTT, 1 mM spermine, 50 mM KCl, 0.01% Nonidet P-40, and 1 mM MgCl2. PARP reaction contains 0.1 μCi [3H]NAD+ (200 000 DPM), 1.5 μM NAD+, 150 nM biotinylated NAD+, 1 μg/mL activated calf thymus, and 1?5 nM PARP-1. Autoreactions utilizing SPA bead-based detection are carried out in 50 μL volumes in white 96-well plates. Compounds (e.g., MK-4827) are prepared in 11-point serial dilution in 96-well plate, 5 μL/well in 5% DMSO/Water (10× concentrated). Reactions are initiated by adding first 35 μL of PARP-1 enzyme in buffer and incubating for 5 min at room temperature and then 10 μL of NAD+ and DNA substrate mixture. After 3 h at room temperature, these reactions are terminated by the addition of 50 μL of streptavidin-SPA beads (2.5 mg/mL in 200 mM EDTA, pH 8). After 5 min, they are counted using a TopCount microplate scintillation counter. IC50 data is determined from inhibition curves at various substrate concentrations[1].
Cell Research IL-1β-stimulated A549 cells (5×106/ml) are pre-incubated with MK-886 (MK, 33 μM), indomethacin (Indo, 10 μM), celecoxib (Cele, 5 μM) or vehicle (DMSO) for 15 min prior to the addition of 30 μM arachidonic acid. After 15 min at 37 °C, the amount of released 6-keto PGF1α was assessed by ELISA as described in the Materials and methods section. (Only for Reference)
Synonyms MK886, L 663536, MK 886
Molecular Weight 472.08
Formula C27H34ClNO2S
CAS No. 118414-82-7


Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

Ethanol: 2.4 mg/mL (5 mM)

DMSO: 47.2 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Koeberle A, et al. Eur J Pharmacol. 2009, 608(1-3):84-90. 2. Imbesi M, et al. Brain Res. 2007, 1147:148-53. 3. Kehrer JP, et al. Biochem J. 2001, 356(Pt 3):899-906.


1. Wang M, Luo W, Yu T, et al. Corynoline protects ang II-induced hypertensive heart failure by increasing PPARα and Inhibiting NF-κB pathway. Biomedicine & Pharmacotherapy. 2022, 150: 113075 2. Wang, Yuan, et al. Hippocampal PPARα plays a role in the pharmacological mechanism of vortioxetine, a multimodal-acting antidepressant. Frontiers in Pharmacology. 12 (2021). 3. Gao S, Zhang X, Xu H, et al. Promoting the hippocampal PPARα expression participates in the antidepressant mechanism of reboxetine, a selective norepinephrine reuptake inhibitor. Behavioural Brain Research. 2021: 113535.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Compound Library Preclinical Compound Library GPCR Compound Library HIF-1 Signaling Pathway Compound Library Anti-Cardiovascular Disease Compound Library Inhibitor Library Immunology/Inflammation Compound Library Anti-Metabolism Disease Compound Library Anti-Cancer Active Compound Library Anti-Breast Cancer Compound Library

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MK-886 118414-82-7 DNA损伤和修复 G蛋白偶联受体 代谢 凋亡 免疫与炎症 神经科学 Apoptosis COX FLAP Leukotriene Receptor PPAR leukotriene 5-LO activating protein non-competitive L-663536 L663536 keratin-1 Inhibitor biosynthesis MK886 PPARα L 663536 MK 886 inhibit 5-LOX Peroxisome proliferator-activated receptors inhibitor