Chemical Name: 5-(2-Fluoro-4-pyridinyl)-2-(phenylmethoxy)-N-3-pyridinylbenzamide
Biological ActivityPotent LRRK2 inhibitor (IC50 values are 8.9 and 10.1 nM for LRRK2[G2019S] mutant and wild-type LRRK2 respectively). Displays selectivity for LRRK2 over a panel of 460 other kinases. Blocks Ser910 and Ser935 phosphorylation in vitro and in peripheral tissues in vivo. Brain penetrant.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substituent-N-arylbenzamide LRRK2 kinase inhibitor.
Reith et al.
Citations for GSK2578215A
The citations listed below are publications that use Tocris products. Selected citations for GSK2578215A include:
7 Citations: Showing 1 - 7
Inhibitor treatment of peripheral mononuclear cells from Parkinson's disease patients further validates LRRK2dephosphorylation as a pharmacodynamic biomarker.
Authors: Perera Et al.
Scientific Reports 2016;6:31391
LRRK2 phosphorylates pre-synaptic N-ethylmaleimide sensitive fusion (NSF) protein enhancing its ATPase activity and SNARE complex disassembling rate.
Authors: Belluzzi Et al.
Mol Neurodegener 2016;11:1
Leucine-Rich Repeat Kinase 2 (LRRK2) phosphorylates p53 and induces p21(WAF1/CIP1) expression.
Authors: Ho Et al.
Mol Brain 2015;8:54
Leucine-rich repeat kinase 2 positively regulates inflammation and down-regulates NF-κB p50 signaling in cultured microglia cells.
Authors: Russo Et al.
LRRK2 kinase activity regulates synaptic vesicle trafficking and neurotransmitter release through modulation of LRRK2 macro-molecular complex.
Authors: Cirnaru Et al.
Front Mol Neurosci 2014;7:49
The LRRK2 inhibitor GSK2578215A induces protective autophagy in SH-SY5Y cells: involvement of Drp-1-mediated mitochondrial fission and mitochondrial-derived ROS signaling.
Authors: Saez-Atienzar Et al.
Cell Death Dis. 2014;5:e1368
Inhibition of LRRK2 kinase activity stimulates macroautophagy.
Authors: Manzoni Et al.
Biochim Biophys Acta 2013;1833:2900
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