Chemical Name: 5,11-Dihydro-2-[[2-methoxy-4-[[4-(4-methyl-1-piperazinyl)-1-piperidinyl]carbonyl]phenyl]amino]-5,11-dimethyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one
Biological ActivityPotent and selective inhibitor of leucine-rich repeat kinase 2 (LRRK2). Inhibits both G2019S mutant and wild-type LRRK2 kinase activity (IC50 values are 6 and 13 nM respectively). Causes dephosphorylation, ubiquitination and degradation of LRRK2. Inhibits IFN-γ-induced monocyte maturation in vitro.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
LRRK2 Dephosphorylation increases its ubiquitination.
Zhao et al.
Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2.
Deng et al.
Regulation of LRRK2 expression points to a functional role in human monocyte maturation.
Thévenet et al.
PLoS One, 2011;6:e21519
Citations for LRRK2-IN-1
The citations listed below are publications that use Tocris products. Selected citations for LRRK2-IN-1 include:
6 Citations: Showing 1 - 6
Brain injury induces HIF-1α-dependent transcriptional activation of LRRK2 that exacerbates brain damage.
Authors: Bae Et al.
Cell Death Dis 2018;9:1125
LRRK2 interacts with ATM and regulates Mdm2-p53 cell proliferation axis in response to genotoxic stress.
Authors: Chen Et al.
Hum Mol Genet 2017;26:4494
Phosphorylation of amyloid precursor protein by mutant LRRK2 promotes AICD activity and neurotoxicity in Parkinson's disease.
Authors: Chen Et al.
Sci Signal 2017;10
LRRK2 kinase activity and biology are not uniformly predicted by its autophosphorylation and cellular phosphorylation site status.
Authors: Reynolds Et al.
Front Mol Neurosci 2014;7:54
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
Phosphorylation of LRRK2 by casein kinase 1α regulates trans-Golgi clustering via differential interaction with ARHGEF7.
Authors: Chia Et al.
BMC Cancer 2014;5:5827
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