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Beschreibung

An orally bioavailable benzofuranylallylamine compound that acts as a potent, active site targeting, competitive and reversible inhibitor of 2,3-oxidosqualene:lanosterol cyclase activity (OSC, IC50 ~6.5 nM against mammalian) and reduces cholesterol synthesis (IC50 ~1.5 nM in HepG2 cells) with minimal buildup of both dioxidosqualene and monooxidosqualene. Downregulates 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase mRNA and synthesis, and exerts less adverse effects in animal models than Statins. Shown to preferentially enhance the DNA-binding affinity of mutant p53 and arrest the growth of human breast cancer cells (IC50 ~10 microM)., An orally bioavailable benzofuranylallylamine compound that acts as a potent, active site targeting, competitive and reversible inhibitor of 2,3-oxidosqualene:lanosterol cyclase activity (OSC, IC50 ~ 6.5 nM against mammalian) and reduces cholesterol synthesis (IC50 ~ 1.5 nM in HepG2 cells) with minimal buildup of both dioxidosqualene and monooxidosqualene. Downregulates 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase mRNA and synthesis, and exerts less adverse effects in animal models than Statins. Shown to preferentially enhance the DNA-binding affinity of mutant p53 and arrest the growth of human breast cancer cells (IC50 ~ 10 microM).