性能参数

产品名称

LRRK2-IN-1

规格

10mM (in 1mL DMSO) 10mg 50mg 100mg

货号

GOY-Y2862

 含量

>98.00%

CAS

1234480-84-2

别名

LRRK 2-IN-1

化学名

2-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]anilino]-5,11-dimethylpyrimido[4,5-b][1,4]benzodiazepin-6-one

分子式

C31H38N8O3

分子量

分子量 570.7

溶解度

≥ 28.55mg/mL in DMSO, ≥ 57.2mg/mL in EtOH

储存条件

Store at -20°C

General tips

用途

仅供科研

价格

电询

详细内容

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]

环己硫醇  98%  甲醇中正十六烷标准溶液 1000μg/ml

邻苯二酚 AR,99.0%  三聚氰酸 98%

正癸烷 standard for GC, ≥99.5% (GC)  三聚氰酸 分析标准品, ≥99.0% (HPLC)

正癸烷 99%  乙基汞标准溶液 10μg/ml，溶剂：甲苯

正癸烷 98%  红外光度法测油标准溶液每套含3瓶

正癸烷 分析标准品，≥99.8% (GC)  正十六烷标准溶液1000mg/L,溶剂:四氯化碳

Congo Red50mg>98.00%Cas No. 573-58-0C32H22N6Na2O6S2

Conantokin-T500μg>98.00%Cas No. 127476-26-0C110H175N31O45S

Conantokin G500μg>98.00%Cas No. 93438-65-4C88H138N26O44

Cyfluthrin100 mg>98.00%Cas No. 68359-37-5C22H18Cl2FNO3

Darodipine (PY 108-068)1mg>98.00%Cas No. 72803-02-2C19H21N3O5

D-CPP-ene10mg>98.00%Cas No. 117414-74-1C8H15N2O5P

DHBP dibromide100mg>98.00%Cas No. 6159-05-3C24H38Br2N2