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.[1]
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)
Questions
Reviews
★★★★★ No rating value
Active Filters
Il team dei nostri ricercatori vanta grande esperienza in tutte le aree della ricerca quali Life Science, scienza dei materiali, sintesi chimica, cromatografia, discipline analitiche, ecc..
