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LRRK2-IN-1 LRRK2 inhibitor,cell-permeable and ATP competitive

Catalog No.A3558
Size Price Stock Qty
10mM (in 1mL DMSO)
$127.00
In stock
10mg
$85.00
In stock
50mg
$320.00
In stock
100mg
$470.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Chen J, Su P, et al. "Role of LRRK2 in manganese-induced neuroinflammation and microglial autophagy." Biochem Biophys Res Commun. 2018 Mar 25;498(1):171-177. PMID:29408508

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Chemical structure

LRRK2-IN-1

Related Biological Data

LRRK2-IN-1

Biological Activity

Description LRRK2-IN-1 is a potent and selective inhibitor of leucine-rich repeat kinase 2 (LRRK2) with IC50 values of 13 nM and 6 nM for wild-type LRRK2 and G2019S mutant LRRK2, respectively.
Targets wild-type LRRK2 G2019S mutant LRRK2        
IC50 13 nM 6 nM        

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Chemical Properties

Cas No. 1234480-84-2 SDF Download SDF
Synonyms LRRK 2-IN-1
Chemical Name 2-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]anilino]-5,11-dimethylpyrimido[4,5-b][1,4]benzodiazepin-6-one
Canonical SMILES CN1CCN(CC1)C2CCN(CC2)C(=O)C3=CC(=C(C=C3)NC4=NC=C5C(=N4)N(C6=CC=CC=C6C(=O)N5C)C)OC
Formula C31H38N8O3 M.Wt 570.7
Solubility ≥28.55mg/mL in DMSO, ≥57.2mg/mL in EtOH, <2.87mg/mL in H2O Storage Store at -20°C
Physical Appearance A solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

LRRK2-IN-1 is a potent and selective inhibitor of LRRK2 with IC50 value of 13 nM. [1]
LRRK2 (Leucine-rich repeat kinase 2) is also known dardarin. LRRK2 belongs to the leucine-rich repeat kinase family. LRRK2 mostly located in the cytoplasm, however, it also associates with outer membrane of the mitochondrial. LRRK2 interacts with parkin at the C-terminal R2 RING finger domain. Parkin interacted with LRRK2 at the COR domain. LRRK2 mutation will induce apoptotic cell death of neuroblastoma cells. Expression of LRRK2 mutants has a close relationship with autosomal dominant Parkinson's disease. The LRRK2 Gly2019Ser mutation is a common cause of familial Parkinson's disease. The Gly2019Ser mutation has been proved to cause Parkinson's disease, even though it is a small number of LRRK2 mutations. LRRK2 also has relationship with Crohn's disease by genomewide association studies.
LRRK2-IN-1 dose-dependent inhibit the activity of wild-type and G2019S LRRK2 with IC50 of 0.17 and 0.04μM respectively in HEK293 cells stably expressing GFP tagged wild-type or mutated LRRK2.[2] LRRK2-IN-1 inhibits the activity of both wild-type and G2019S mutant LRRK2 with IC 50 values of 13 nM and 6 nM respectively in vitro enzyme assay with 0.1 mM ATP. LRRK2-IN-1 competed with ATP. LRRK2-IN-1 has a selective profile compared with other 442 diverse kinases and it has no inhibition effect with LRRK1. LRRK2-IN-1 induced endogenous LRRK2 phosphorylation in lymphoblastoid cells. LRRK2-IN-1 also induced Ser910/Ser935 dephosphorylation of LRRK2 in mice kidney at 100 mg/kg.[1]
References:
[1].    Deng X, Dzamko N, Prescott A, Davies P, Liu Q, Yang Q, Lee JD, Patricelli MP, Nomanbhoy TK, Alessi DR et al: Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2. Nat Chem Biol, 7(4):203-205.
[2].    Hermanson SB, Carlson CB, Riddle SM, Zhao J, Vogel KW, Nichols RJ, Bi K: Screening for novel LRRK2 inhibitors using a high-throughput TR-FRET cellular assay for LRRK2 Ser935 phosphorylation. PLoS One, 7(8):e43580.