A selective LRRK2 inhibitor
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LRRK2-IN-1

Item No. 18094

Technical Information
Formal 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
CAS Number
1234480-84-2
Synonyms
  • Leucine-rich repeat kinase 2 IN-1
Molecular Formula
C31H38N8O3
Formula Weight
Purity
≥95%
A crystalline solid
DMF: 20 mg/mlDMSO: 16 mg/mlEthanol: 25 mg/mlEthanol:PBS(pH 7.2) (1:1): 0.5 mg/ml
λmax
209, 309 nm
SMILES
CN1CCN(C2CCN(C(C3=CC(OC)=C(NC4=NC=C(N(C)C(C5=CC=CC=C5N6C)=O)C6=N4)C=C3)=O)CC2)CC1
InChi Code
InChI=1S/C31H38N8O3/c1-35-15-17-38(18-16-35)22-11-13-39(14-12-22)29(40)21-9-10-24(27(19-21)42-4)33-31-32-20-26-28(34-31)36(2)25-8-6-5-7-23(25)30(41)37(26)3/h5-10,19-20,22H,11-18H2,1-4H3,(H,32,33,34)
InChi Key
IWMCPJZTADUIFX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    LRRK2-IN-1 is a potent inhibitor of LRRK2 that inhibits both wild-type and G2019S mutant LRRK2 (IC50s = 13 and 6 nM, respectively).1 It is selective for LRRK2 over a large panel of other kinases. LRRK2-IN-1 treatment causes dephosphorylation of LRRK2, leading to its dissociation from 14-3-3 proteins, ubiquitination, and degradation.1,2 Inhibitors of LRRK2, including LRRK2-IN-1, stimulate macroautophagy in H4 neuroglioma cells.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Deng, X., Dzamko, N., Prescott, A., et alCharacterization of a selective inhibitor of the Parkinson’s disease kinase LRRK2. Nat. Chem. Biol. 7(4), 203-205 (2011).

    2. Zhao, J., Molitor, T.P., Langston, J.W., et alLRRK2 dephosphorylation increases its ubiquitination. Biochem. J. 469, 107-120 (2015).

    3. Manzoni, C., Mamais, A., Dihanich, S., et alInhibition of LRRK2 kinase activity stimulates macroautophagy. Biochem. Biophys. Acta 1833, 2900-2910 (2013).

    Product Citations

    Alavi, M.V. Tau phosphorylation and OPA1 proteolysis are unrelated events: Implications for Alzheimer’s Disease. Biochim. Biophys. Acta Mol. Cell Res. 1868(12), 119116 (2021).