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CAS No.: 1234480-84-2

LRRK2-IN-1 Catalog No. CSN15891

Synonyms: Leucine-rich repeat kinase 2 IN-1

LRRK2-IN-1 is a potent and selective LRRK2 inhibitor with IC50 values of 6 and 13 nM for G2019S mutant and wild-type LRRK2, respectively.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Mutations in the leucine-rich repeat kinase-2 (LRRK2) gene is tightly linked to Parkinson's disease (PD) as its missense mutation, G2019S, is frequently found in not only familial but also sporadic PD. LRRK-2IN1 inhibits both wild-type and G2019S mutant LRRK2 kinase activity with IC₅₀ values of 13 nM and 6 nM, respectively^[4]. LRRK2-IN-1 at 100 nM and 500 nM could protect against G2019S-associated cellular toxicity and significantly improve cell survival in human SH-SY5Y neuroblastoma cell line transfected with G2019S -LRRK2 along. It was also found that treatment of LRRK2-IN1 during both pre- and post-symptomatic stages significantly protect dopamine neurons against neurodegeneration caused by G2019S in C. elegans ^[5]. AsPC-1 cells treated with 0.5 μM- and 5.0 μM-LRRK2-IN-1 showed decreased expression of epithelial-to-mesenchymal transition (EMT) factors and WNT1, increased expression of E-cadherin. Consistently, there was a dose-dependent reduction in the invasive potential of AsPC-1 cells 24 h post LRRK2-IN-1 treatment, with an approximately 70% decrease in invasive potential following 5 μM treatment. AsPC-1 tumor xenografts injected with LRRK2-IN-1(100 mg/kg, 4weeks) showed more than 50% decreases in tumor volume and weight^[6].
作用机制LRRK2-IN-1 inhibits wild-type and G2019S mutant LRRK2 kinase in an ATP-competitive manner.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
HEK293 cells	-	Function assay	-	Inhibition of LRRK2 G2019S mutant expressed in HEK293 cells using nictide and ATP as substrate, IC50=0.006 μM	22335897
HEK293 cells	0.03-3 μM	Function assay	90 mins	Inhibition of wild-type LRRK2 phosphorylation at Ser935 expressed in HEK293 cells at 0.03 to 3 uM after 90 mins by immunoblot analysis	22335897
lymphoblastoid cells	0.03 to 3 uM	Function assay	90 mins	Inhibition of LRRK2 in human lymphoblastoid cells assessed as inhibition of Ser910 autophosphorylation at 0.03 to 3 uM after 90 mins by immunoblot method	22863203

动物研究
剂量
Mice: 100 mg/kg^[3] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 100 mg/kg^[3] (i.p.)
给药途径	i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7523 mL
- 8.7614 mL
- 17.5228 mL
- 5 mM
- 0.3505 mL
- 1.7523 mL
- 3.5046 mL
- 10 mM
- 0.1752 mL
- 0.8761 mL
- 1.7523 mL

技术信息

CAS号

1234480-84-2

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C31H38N8O3

运输

蓝冰

分子量

570.69

别名

Leucine-rich repeat kinase 2 IN-1

溶解度

DMSO	500.0 mg/mL (876.1 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+30% PEG300+water	10 mg/mL	clear
PO	0.5% CMC-Na	13 mg/mL	suspension

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