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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.
Sold under license from the Dana-Farber Cancer Institute.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 570.09. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.75 mL||8.77 mL||17.54 mL|
|5 mM||0.35 mL||1.75 mL||3.51 mL|
|10 mM||0.18 mL||0.88 mL||1.75 mL|
|50 mM||0.04 mL||0.18 mL||0.35 mL|
References are publications that support the biological activity of the product.
Deng et al (2011) Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2. Nat.Chem.Biol. 7 203 PMID: 21378983
Zhao et al (2015) LRRK2 Dephosphorylation increases its ubiquitination. Biochem.J. 469 107 PMID: 25939886
Thévenet et al (2011) Regulation of LRRK2 expression points to a functional role in human monocyte maturation. PLoS One 6 e21519 PMID: 21738687
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Keywords: LRRK2-IN-1, LRRK2-IN-1 supplier, parkinsons, disease, lrrk2, leucine-rich, repeat, kinase, 2, dardarin, parkinson's, LRRK2, 4273, Tocris Bioscience
6 Citations for LRRK2-IN-1
Citations are publications that use Tocris products. Selected citations for LRRK2-IN-1 include:
Chia et al (2014) Phosphorylation of LRRK2 by casein kinase 1α regulates trans-Golgi clustering via differential interaction with ARHGEF7. BMC Cancer 5 5827 PMID: 25500533
Bae et al (2018) Brain injury induces HIF-1α-dependent transcriptional activation of LRRK2 that exacerbates brain damage. Cell Death Dis 9 1125 PMID: 30420654
Chen et al (2017) LRRK2 interacts with ATM and regulates Mdm2-p53 cell proliferation axis in response to genotoxic stress. Hum Mol Genet 26 4494 PMID: 28973420
Chen et al (2017) Phosphorylation of amyloid precursor protein by mutant LRRK2 promotes AICD activity and neurotoxicity in Parkinson's disease. Sci Signal 10 PMID: 28720718
Saez-Atienzar et al (2014) The LRRK2 inhibitor GSK2578215A induces protective autophagy in SH-SY5Y cells: involvement of Drp-1-mediated mitochondrial fission and mitochondrial-derived ROS signaling. Cell Death Dis. 5 e1368 PMID: 25118928
Reynolds et al (2014) LRRK2 kinase activity and biology are not uniformly predicted by its autophosphorylation and cellular phosphorylation site status. Front Mol Neurosci 7 54 PMID: 25009464
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
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Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.