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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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:
10 Citations: Showing 1 - 10
Brain injury induces HIF-1α-dependent transcriptional activation of LRRK2 that exacerbates brain damage.
Authors: Bae Et al.
Cell Death Dis 2018;9:1125
Leucine-rich repeat kinase 2 controls protein kinase A activation state through phosphodiesterase 4.
Authors: Russo Et al.
J Neuroinflammation 2018;15:297
RAB7L1-Mediated Relocalization of LRRK2 to the Golgi Complex Causes Centrosomal Deficits via RAB8A.
Authors: Madero-Pérez Et al.
Front Mol Neurosci 2018;11
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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