Catalog # Availability Size / Price Qty
LRRK2-IN-1 | CAS No. 1234480-84-2 | LRRK2 Inhibitors
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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%

Product Details
Citations (7)

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

Soluble to 100 mM in DMSO and to 100 mM in ethanol
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.

Additional Information

Licensing Caveats:
Sold under license from the Dana-Farber Cancer Institute.

Background References

  1. 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):.
  2. 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.
  3. LRRK2 Dephosphorylation increases its ubiquitination.
    Zhao et al.
    Biochem.J., 2015;469:107
  4. Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2.
    Deng et al.
    Nat.Chem.Biol., 2011;7:203
  5. 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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