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DYRK1A、DYRK2、CLK1和CLK3的抑制剂(IC50分别为0.04、0.035、0.015和4.5µM);GSK3α/β和Pim1的抑制剂(IC50分别为0.41和4.1µM);0.1-10µM时可抑制人类微血管内皮细胞中TNF-α诱导的SRp75和SRp55磷酸化;调节合成CLK1小基因的替代前RNA剪接;在阿尔茨海默病样毒性小鼠模型中防止淀粉样蛋白-β25-35诱导的脂质过氧化和海马中ROS积累;在相同模型中防止淀粉样蛋白-β25-35诱导的记忆缺陷,浓度为0.4、1.2和4µg。An inhibitor of DYRK1A, DYRK2, CLK1, and CLK3 (IC50s = 0.04, 0.035, 0.015, and 4.5 µM, respectively); an inhibitor of GSK3α/β and Pim1 (IC50s = 0.41and 4.1 µM, respectively); inhibits TNF-α-induced SRp75 and SRp55 phosphorylation in human microvascular endothelial cells at 0.1-10 µM; modulates alternative pre-RNA splicing of a synthetic CLK1 minigene; prevents amyloid-β 25-35-induced lipid peroxidation and ROS accumulation in the hippocampus in a mouse model of Alzheimer's disease-like toxicity; prevents amyloid-β 25-35-induced memory deficits in the same model at 0.4, 1.2, and 4 µg.
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Leucettine L41
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