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Beschreibung

A cell-permeable, non-Hemicholinium-3 derivative and choline-competitive choline kinase-alpha inhibitor. It is demonstrated to inhibit endogenous choline kinase activity, dose-dependently, between 1-10 µ,M, and dose-dependently decrease phosphocholine concentrations, as well as levels of downstream choline metabolites, including phosphatidylcholine and phosphatidic acid in HeLa cells. At 10 µ,M, it is also shown to attenuate MAPK and PI3K/AKT signaling, and disrupt the actin cytoskeleton and membrane ruffling, consistent with siRNA choline kinase-alpha transfection. This compound exhibits dose-dependent suppression of cell growth in six tumor cell lines (IC50 = 5-10 µ,M), in vitro. Furthermore, it is shown to suppress tumor growth in a mouse model by 48% at 0.08 mg/g daily dose for 8 days without obvious toxicity, in vivo., A cell-permeable, non-Hemicholinium-3 derivative and choline-competitive choline kinase-alpha inhibitor. It is demonstrated to inhibit endogenous choline kinase activity, dose-dependently, between 1-10 µ,M, and dose-dependently decrease phosphocholine concentrations, as well as levels of downstream choline metabolites, including phosphatidylcholine and phosphatidic acid in HeLa cells. At 10 µ,M, it is also shown to attenuate MAPK and PI3K/AKT signaling, and disrupt the actin cytoskeleton and membrane ruffling, consistent with siRNA choline kinase-&alpha transfection. This compound exhibits dose-dependent suppression of cell growth in six tumor cell lines (IC50 = 5-10 µ,M), in vitro. Furthermore, it is shown to suppress tumor growth in a mouse model by 48% at 0.08 mg/g daily dose for 8 days without obvious toxicity, in vivo.