MK-886

For research use only.

Catalog No.S8236 Synonyms: L-663,536

3 publications

MK-886 Chemical Structure

Molecular Weight(MW): 472.08

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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Selleck's MK-886 has been cited by 3 publications

1 Customer Review

  • HepG2 cells were subjected to the PPARα antagonist MK886 (20 μM) or the PPARγ antagonist T0070907 (20 μM) for 2 h, followed by N15 (100 μM) treatment for an additional 12h.

    Eur J Pharmacol, 2018, 826:1-8. MK-886 purchased from Selleck.

Purity & Quality Control

Choose Selective Lipoxygenase Inhibitors

Biological Activity

Description MK-886 is an inhibitor of leukotriene biosynthesis, inhibiting 5-lipoxygenase-activating protein (FLAP). It is also a moderately potent PPARα antagonist.
Targets
5-lipoxygenase-activating protein (FLAP) [1] PPARα [3] COX-1 [1] COX-2 [1]
8 μM 58 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 1.13.11.34) 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].

Protocol

Cell Research:

[1]

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  • Cell lines:  A549 cells
  • Concentrations: 33 μM
  • Incubation Time: 15 min
  • Method:

    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)
Animal Research:

[2]

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  • Animal Models: Male C57BL/6J mice
  • Dosages: 3 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 94 mg/mL (199.11 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 472.08
Formula

C27H34ClNO2S

CAS No. 118414-82-7
Storage powder
in solvent
Synonyms L-663,536
Smiles CC(C)C1=CC=C2[N](CC3=CC=C(Cl)C=C3)C(=C(SC(C)(C)C)C2=C1)CC(C)(C)C(O)=O

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID