MK-886

SKU: orb1300370

Description

MK-886 (L 663536) is a small molecule that acts as a dual-function agent, primarily known as a 5-lipoxygenase-activating protein (FLAP) inhibitor that blocks leukotriene biosynthesis. It also serves as a moderate PPARα antagonist. This compound has been utilized in research exploring inflammation, asthma, and metabolic diseases in both cellular and animal models.

Research Area

Immunology & Inflammation

Key Properties

• CAS Number: 118414-82-7
• MW: 472.1
• Purity: >98%
• Formula: C₂₇H₃₄ClNO₂S
• SMILES: CC(C)c1ccc2n(Cc3ccc(Cl)cc3)c(CC(C)(C)C(O)=O)c(SC(C)(C)C)c2c1
• Target: PPAR
• Solubility: Soluble in DMSO (up to 40 mg/ml).

Bioactivity

• Target IC50:
  COX-2:58 μM|COX-1:8 μM
• 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.
• 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.
• 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)

Storage & Handling

• Storage: RT
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

L-663,536

Compound Identifiers

PubChem CID

3651377