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品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 15 mg/mL, clear
儲存溫度
2-8°C
InChI
1S/C24H18FN3O2/c25-23-14-19(10-12-27-23)18-8-9-22(30-16-17-5-2-1-3-6-17)21(13-18)24(29)28-20-7-4-11-26-15-20/h1-15H,16H2,(H,28,29)
InChI 密鑰
WCIGMFCFPXZRMQ-UHFFFAOYSA-N
生化/生理作用
GSK2578215A is a potent inhibitor of leucine-rich repeat kinase-2 (LRRK2) also known as dardarin or PARK8, a kinase with mutations linked to Parkinson′s disease. Because the most common mutation, G2019S, enhances LRRK2 kinase activity, it is hoped that LRRK2 inhibitors may be useful in treating the disease. GSK2578215A inhibited both wild-type and G2019S mutant LRRK2 kinase activity with IC50s of 10.9 and 8.9 nM respectively. It has good blood-brain barrier (BBB) permeability with a high ratio of brain to plasma distribution in mice.
GSK2578215A stimulates mitochondrial fragmentation, autophagy and mitophagy.
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
The LRRK2 inhibitor GSK2578215A induces protective autophagy in SH-SY5Y cells: involvement of Drp-1-mediated mitochondrial fission and mitochondrial-derived ROS signaling
Cell Death & Disease, 5(8), e1368-e1368 (2014)
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