LRRK2-IN-1

inquiry

Cat No.

CEI-1401

Description

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

Product Overview

LRRK2-IN-1 is a potent and selective inhibitor of LRRK2 with IC50 value of 13 nM. 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 Parkinsons disease. The LRRK2 Gly2019Ser mutation is a common cause of familial Parkinsons disease. The Gly2019Ser mutation has been proved to cause Parkinsons disease, even though it is a small number of LRRK2 mutations. LRRK2 also has relationship with Crohns 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. 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.

CAS_No

1234480-84-2

Molecular Weight

570.7

Purity

0.9801

Storage

Store at -20°C

Synonyms

LRRK 2-IN-1

Targets

LRRK2

IC50

13 nM; 6 nM

Molecular Formula

C31H38N8O3

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

Solubility

Soluble in DMSO > 10 mM

Shipping Conditions

Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request

Name:

Email *

Phone:*

Company/Institution:

Country or Region:

Quantity:

Services & Products Interested *

Project Description:

Our Products Cannot Be Used As Medicines Directly For Personal Use.

Products

Online Inquiry