Catalog Number: 4273
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.
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.
Additional Information
Licensing Caveats:
Sold under license from the Dana-Farber Cancer Institute.
Background References
  1. Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2.
    Deng et al.
    Nat.Chem.Biol., 2011;7:203
  2. LRRK2 Dephosphorylation increases its ubiquitination.
    Zhao et al.
    Biochem.J., 2015;
Citations:

The citations listed below are publications that use Tocris products. Selected citations for LRRK2-IN-1 include:

3 Citations: Showing 1 - 3
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  1. 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
  2. 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
  3. 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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