MK 886

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Description: Inhibitor of 5-lipoxygenase-activating protein (FLAP)
Alternative Names: L-663,536
Chemical Name: 1-[(4-Chlorophenyl)methyl]-3-[(1,1-dimethylethyl)thio]-α,α-dimethyl-5-(1-methylethyl)-1H-Indole-2-propanoic acid
Purity: ≥98% (HPLC)
Citations (11)
Literature (2)

Biological Activity for MK 886

MK 886 is a potent inhibitor of 5-lipoxygenase-activating protein (FLAP) (IC50 = 30 nM for inhibition of [125I]-L-691,678 photoaffinity labelling). Inhibits leukotriene biosynthesis (IC50 = 3 nM in human polymorphonuclear leukocytes). Also moderately potent PPARα antagonist (IC50 = 0.5-1 μM). Orally active in vivo.

Technical Data for MK 886

M. Wt 472.08
Formula C27H34ClNO2S
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 118414-82-7
PubChem ID 3651377
Smiles ClC(C=C3)=CC=C3CN(C(CC(C)(C(O)=O)C)=C2SC(C)(C)C)C1=C2C=C(C(C)C)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for MK 886

Solvent Max Conc. mg/mL Max Conc. mM
ethanol 2.36 5
DMSO 47.21 100

Preparing Stock Solutions for MK 886

The following data is based on the product molecular weight 472.08. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.12 mL 10.59 mL 21.18 mL
5 mM 0.42 mL 2.12 mL 4.24 mL
10 mM 0.21 mL 1.06 mL 2.12 mL
50 mM 0.04 mL 0.21 mL 0.42 mL

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Product Datasheets for MK 886

Certificate of Analysis / Product Datasheet
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References for MK 886

References are publications that support the biological activity of the product.

Dixon et al (1990) Requirement of a 5-lipoxygenase-activating protein for leukotriene synthesis. Nature 343 282 PMID: 2300173

Gillard et al (1989) 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. Can.J.Physiol.Pharmacol. 67 456 PMID: 2548691

Kehrer et al (2001) Inhibition of peroxisome-proliferator-activated receptor (PPAR)α by MK886. Biochem.J. 356 899 PMID: 11389700

Mancini et al (1992) 5-Lipoxygenase-activating protein is the target of a novel hybrid of two classes of leukotriene biosynthesis inhibitors. Mol.Pharmacol. 41 267 PMID: 1538707

If you know of a relevant reference for MK 886, please let us know.

View Related Products by Product Action

View all Lipoxygenase Inhibitors

Keywords: MK 886, MK 886 supplier, Inhibitor, 5-lipoxygenase-activating, protein, FLAP, PPARα, PPARalpha, antagonists, inhibitors, inhibits, Oxygenases, Oxidases, leukotrienes, eicosanoids, biosynthesis, Peroxisome, Proliferator-activated, PPARs, MK886, L663536, 5-LOX, L-663,536, Lipoxygenase, Receptors, Leukotriene, and, Related, 1311, Tocris Bioscience

11 Citations for MK 886

Citations are publications that use Tocris products. Selected citations for MK 886 include:

Eisele et al (2013) The peroxisome proliferator-activated receptor γ coactivator 1α/β (PGC-1) coactivators repress the transcriptional activity of NF-κB in skeletal muscle cells. J Biol Chem 288 2246 PMID: 23223635

Puligheddu et al (2013) PPAR-alpha agonists as novel antiepileptic drugs: preclinical findings. PLoS One 8 e64541 PMID: 23724059

Oguh-Olayinka et al (2019) The Investigation of Lipoxygenases as Therapeutic Targets in Malignant Pleural Mesothelioma. Pathol Oncol Res PMID: 30941737

Vigna et al (2011) Leukotriene B4 mediates inflammation via TRPV1 in duct obstruction-induced pancreatitis in rats. Pancreas 40 708 PMID: 21602738

Do you know of a great paper that uses MK 886 from Tocris? Please let us know.

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Literature in this Area

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