5-Lipoxygenase Inhibitor, MK591 – CAS 147030-01-1 – Calbiochem

Descrição detalhada : 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
Sinónimos : 5-Lipoxygenase Inhibitor, MK591 - CAS 147030-01-1 - Calbiochem; FLAP Inhibitor, MK591, sodium 3-(3-(tert-butylthio)-1-(4-chlorobenzyl)-5-(quinolin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropanoate, L-686,708, MK-0591
Fórmula molecula r: C34H34ClN2NaO3S
Armazenamento : -20C
Embalagem : 1X1EA