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Arachidonic acid and selected other polyunsaturated fatty acids are stereoselectively oxygenated at carbon 5 by the non-heme iron containing enzyme 5-lipoxygenase (5-LO).1 The intervention of a second protein, 5-LO-activating protein (FLAP), is required before 5-LO can become catalytically active.2 MK 886 binds to FLAP with high-affinity and prevents 5-LO activation. MK 886 inhibits leukotriene biosynthesis in leukocytes with an IC50 of 2.5 nM.3 In human whole blood, leukotriene biosynthesis is inhibited by MK 886 with an IC50 of 1.1 µM.
1
Ford-Hutchinson, A.W., Gresser, M., and Young, R.N. 5-Lipoxygenase. Annu Rev Biochem63383-417(1994).
2
Abramovitz, M., Wong, E., Cox, M.E., et al. 5-Lipoxygenase-activating protein stimulates the utilization of arachidonic acid by 5-lipoxygenase. Eur J Biochem215105-111(1993).
3
Dixon, R.A.F., Diehl, R.E., Opas, E., et al. Requirement of a 5-lipoxygenase-activating protein for leukotriene synthesis. Nature343282-284(1990).
Formal Name
1-[(4-chlorophenyl)methyl]-3-[(1,1-dimethylethyl)thio]-α,α-dimethyl-5-(1-methylethyl)-1H-indole-2-propanoic acid, sodium salt
CAS Number
118427-55-7
Molecular Formula
C27H33ClNO2S · Na
Formula Weight
494.1
Formulation
A crystalline solid
Purity
>99%
λmax
226, 289 nm
Stability
1 year
Storage
-20°C
Shipping
Room temperature
in continental US; may vary elsewhere
Ford-Hutchinson, A.W., Gresser, M., and Young, R.N. 5-Lipoxygenase. Annu Rev Biochem63383-417(1994).
. . Can J Physiol Pharmacol67456(1989).
Dixon, R.A.F., Diehl, R.E., Opas, E., et al. Requirement of a 5-lipoxygenase-activating protein for leukotriene synthesis. Nature343282-284(1990).
Abramovitz, M., Wong, E., Cox, M.E., et al. 5-Lipoxygenase-activating protein stimulates the utilization of arachidonic acid by 5-lipoxygenase. Eur J Biochem215105-111(1993).