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Submit ReviewLRRK2-IN-1
Description: Potent and selective LRRK2 inhibitor
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% (HPLC)
Biological Activity for LRRK2-IN-1
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.
Licensing Information
Sold under license from the Dana-Farber Cancer Institute.
Compound Libraries for LRRK2-IN-1
LRRK2-IN-1 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for LRRK2-IN-1
| M. Wt | 570.69 |
| Formula | C31H38N8O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1234480-84-2 |
| PubChem ID | 46843906 |
| InChI Key | IWMCPJZTADUIFX-UHFFFAOYSA-N |
| Smiles | O=C2C3=C(C=CC=C3)N(C)C1=NC(NC4=C(OC)C=C(C(N5CCC(N6CCN(C)CC6)CC5)=O)C=C4)=NC=C1N2C |
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.
Solubility Data for LRRK2-IN-1
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 57.01 | 100 | |
| ethanol | 57.01 | 100 |
Preparing Stock Solutions for LRRK2-IN-1
The following data is based on the product molecular weight 570.69. 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 | 8.76 mL | 17.52 mL |
| 5 mM | 0.35 mL | 1.75 mL | 3.5 mL |
| 10 mM | 0.18 mL | 0.88 mL | 1.75 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.35 mL |
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Product Datasheets for LRRK2-IN-1
References for LRRK2-IN-1
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
If you know of a relevant reference for LRRK2-IN-1, please let us know.
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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
7 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
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
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
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
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
Elisa et al (2019) Leucine-rich repeat kinase 2 phosphorylation on synapsin I regulates glutamate release at pre-synaptic sites. J Neurochem 150 264-281 PMID: 31148170
Do you know of a great paper that uses LRRK2-IN-1 from Tocris? Please let us know.
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Parkinson's Disease Poster
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.