MK-886

BML-EI266

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FLAP inhibitor

Inhibitor of PPARα activation. Inhibits 5-lipoxygenase-activating protein (FLAP) and leukotriene biosynthesis. Binds to FLAP with high affinity and prevents the activation of 5-lipoxygenase. IC₅₀’s for leukotriene biosynthesis: 2.5 nM in intact leukocytes; 1.1 µM in whole blood. Induces apoptosis through the mitochondrial pathway.

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Product Details

Alternative Name	L-663,536, 3-[1-(p-Chlorobenzyl)-5-(isopropyl)-3-t-butylthioindol-2-yl]-2,2-dimethylpropanoic acid . Na
Appearance	White solid.
CAS	118414-82-7
Couple Target	FLAP, PPAR
Couple Type	Inhibitor
Formula	C₂₇H₃₃ClNO₂S·Na
MW	494.0
Purity	≥98% (HPLC)
Solubility	Soluble in 100% ethanol (25mg/ml) or DMSO (25mg/ml).

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. Stable for at least 1 year after receipt when stored, as supplied, at room temperature. Prepare fresh solutions daily.
Long Term Storage	Ambient
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

Peroxisome proliferator-activated receptorα agonists differentially regulate inhibitor of DNA binding expression in rodents and human cells: González, M. d. e. l. C., Corton, J. C., et al.; PPAR Res. 2012, 483536 (2012), Abstract
PPARalpha agonist fenofibrate suppresses tumor growth through direct and indirect angiogenesis inhibition: Panigrahy, D., Kaipainen, A., et al.; PNAS 105, 985 (2008), Abstract
Growth inhibition and apoptosis in human Philadelphia chromosome-positive lymphoblastic leukemia cell lines by treatment with the dual PPARalpha/gamma ligand TZD18: Liu, H., Zang, C., et al.; Blood 107, 3683 (2006), Abstract
Leukotriene B4, an activation product of mast cells, is a chemoattractant for their progenitors: Weller, C. L., Collington, S. J., et al.; J. Exp. Med. 201, 1961 (2005), Abstract
Mitochondria are direct targets of the lipoxygenase inhibitor MK886. A strategy for cell killing by combined treatment with MK886 and cyclooxygenase inhibitors: A. Gugliucci, et al.; J. Biol. Chem. 277, 31789 (2002), Abstract
Inhibition of peroxisome-proliferator-activated receptor (PPAR)alpha by MK886: J.P. Kehrer, et al.; Biochem. J. 356, 899 (2001), Abstract
FLAP: a novel drug target for inhibiting the synthesis of leukotrienes: A.W. Ford-Hutchinson; Trends Pharmacol. Sci. 12, 68 (1991), Abstract
Requirement of a 5-lipoxygenase-activating protein for leukotriene synthesis: R.A. Dixon, et al.; Nature 343, 282 (1990), Abstract
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: J. Gillard, et al.; Can. J. Physiol. Pharmacol. 67, 456 (1989), Abstract

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MK-886

BML-EI266

Product Details

Handling & Storage

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