LRRK2-IN-1
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
Purity: ≥98%
Biological Activity
LRRK2-IN-1 is a potent 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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Parkinson disease-associated LRRK2 G2019S transgene disrupts marrow myelopoiesis and peripheral Th17 response
J Park, JW Lee, SC Cooper, HE Broxmeyer, JR Cannon, CH Kim
J. Leukoc. Biol., 2017;0(0):. -
Phosphorylation of LRRK2 by casein kinase 1alpha regulates trans-Golgi clustering via differential interaction with ARHGEF7.
Chia R, Haddock S, Beilina A, Rudenko I, Mamais A, Kaganovich A, Li Y, Kumaran R, Nalls M, Cookson M
Nat Commun, 2014;5(0):5827. -
LRRK2 Dephosphorylation increases its ubiquitination.
Zhao et al.
Biochem.J., 2015;469:107 -
Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2.
Deng et al.
Nat.Chem.Biol., 2011;7:203 -
Regulation of LRRK2 expression points to a functional role in human monocyte maturation.
Thévenet et al.
PLoS One, 2011;6:e21519
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Citations for LRRK2-IN-1
The citations listed below are publications that use Tocris products. Selected citations for LRRK2-IN-1 include:
7 Citations: Showing 1 - 7
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Leucine-rich repeat kinase 2 phosphorylation on synapsin I regulates glutamate release at pre-synaptic sites.
Authors: Elisa Et al.
J Neurochem 2019;150:264-281
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Brain injury induces HIF-1α-dependent transcriptional activation of LRRK2 that exacerbates brain damage.
Authors: Bae Et al.
Cell Death Dis 2018;9:1125
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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
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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
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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
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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
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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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