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Beschreibung

A cell permeable, bioavailable, 2-indolealkanoic acid derived compound that acts as a highly potent and selective inhibitor of leukotriene biosynthesis (IC50 = 3.1 nM in intact human polymorphonuclear leukocytes). Shown to inhibit 5-lipoxygenase (5-LOX) activity in LNCaP prostate cancer cells by high-affinity binding to 5-lipoxygenase activating protein (FLAP, IC50 = 1.6 nM in a FLAP binding assay). Induces apoptosis in LNCaP cells without blocking PI 3 kinase-Akt or ERK activities. Also shown to induce rapid phosphorylation of c-Jun N-terminal Kinase (JNK) and indirectly block PKCepsilon activity. Suppresses the deposition of Ab1-40 and Ab1-42 peptides in Tg2576 mice (~40 mg/kg/day in diet) with concomitant reduction in the levels of presenilin 1, nicastrin, APH-1 and Pen-2, but without affecting notch signaling. Exhibits desirable pharmacokinetic properties with tmax of 3.3 h and t1/2 = ~12 h.Please note that the molecular weight for this compound is batch-specific due to variable water content., A cell permeable, bioavailable, 2-indolealkanoic acid derived compound that acts as a highly potent and selective inhibitor of leukotriene biosynthesis (IC50 = 3.1 nM in intact human polymorphonuclear leukocytes). Shown to inhibit 5-lipoxygenase (5-LOX) activity in LNCaP prostate cancer cells by high-affinity binding to 5-lipoxygenase activating protein (FLAP, IC50 = 1.6 nM in a FLAP binding assay). Induces apoptosis in LNCaP cells without blocking PI 3 kinase-Akt or ERK activities. Also shown to induce rapid phosphorylation of c-Jun N-terminal Kinase (JNK) and indirectly block PKCepsilon activity. Suppresses the deposition of Ab1-40 and Ab1-42 peptides in Tg2576 mice (~40 mg/kg/day in diet) with concomitant reduction in the levels of presenilin 1, nicastrin, APH-1 and Pen-2, but without affecting notch signaling. Exhibits desirable pharmacokinetic properties with tmax of 3.3 h and t1/2 = ~12 h., MK591, MK0591, 5-LOX inhibitor, 5- Lipoxygenase inhibitor, FLAP