LRRK2-IN-1

Cat. No. 4273

LRRK2-IN-1 C31H38N8O3 [1234480-84-2]

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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 Activity

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.

Licensing Information

Sold under license from the Dana-Farber Cancer Institute.

Technical Data

M.Wt:
570.09
Formula:
C31H38N8O3
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
1234480-84-2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Zhao et al (2015) LRRK2 Dephosphorylation increases its ubiquitination. Biochem.J. 469 107. PMID: 25939886.

Deng et al (2011) Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2. Nat.Chem.Biol. 7 203. PMID: 21378983.

If you know of a relevant reference for this product please let us know.

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.

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.

Do you know of a great paper that uses LRRK2-IN-1 from Tocris? If so please let us know.

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Keywords: LRRK2-IN-1, supplier, parkinsons, disease, lrrk2, leucine-rich, repeat, kinase, 2, dardarin, parkinson's, Tocris Bioscience, LRRK2 Inhibitor products

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