SML0660
GSK2578215A
≥98% (HPLC)
别名:
5-(2-Fluoro-4-pyridinyl)-2-(phenylmethoxy)-N-3-pyridinyl-benzamide
SMILES string
Fc1nccc(c1)c2cc(c(cc2)OCc4ccccc4)C(=O)Nc3cnccc3
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 key
WCIGMFCFPXZRMQ-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 15 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
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 is a potent inhibitor of leucine-rich repeat kinase-2 (LRRK2).
GSK2578215A stimulates mitochondrial fragmentation, autophagy and mitophagy.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_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
Saez-Atienzar S, et al.
Cell Death & Disease, 5(8), e1368-e1368 (2014)
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