5-(2-氟-4-吡啶基)-2-(苯基甲氧基)-N-3-吡啶基苯甲酰

发布者：信康浏览次数：

产品名称:5-(2-氟-4-吡啶基)-2-(苯基甲氧基)-N-3-吡啶基苯甲酰胺

CAS:1285515-21-0

别名：5-(2-氟-4-吡啶基)-2-(苯基甲氧基)-N-3-吡啶基苯甲酰胺;2-(苄氧基)-5-(2-氟吡啶-4-基)-N-(吡啶-3-基)苯甲酰胺

英文名：LRRK2-kinase inhibitor

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生物活性GSK2578215A是一种有效的选择性LRRK2 kinase抑制剂，对LRRK2 (G2019S)和LRRK2 (WT)的IC50分别为8.9 nM 和 10.9 nM。
体外研究GSK2578215A induces a dose-dependent inhibition of Ser910 and Ser935 phosphorylation in both wild-type LRRK2 and LRRK2[G2019S] stably transfected into HEK293 cells, and induces similar dose-dependent Ser910 and Ser935 dephosphorylation of endogenous LRRK2 in mouse Swiss 3T3 cells. In SH-SY5Y cells, GSK2578215A impairs the autophagy flux by altering autophagosome–lysosome fusion, and induces mitophagy though induction of Drp-1-mediated mitochondrial fission and mitochondrial-derived ROS signaling.
体内研究In vivo, GSK2578215A (100 mg/kg i.p.) inhibits Ser910 and Ser935 phosphorylation in mouse spleen and kidney, but not in brain.