LRRK2-IN-1

产品编号: T2246 别名:

5,11-二氢-2-[[2-甲氧基-4-[[4-(4-甲基-1-哌嗪基)-1-哌啶基]羰基]苯基]氨基]-5,11-二甲基-6H-嘧啶并[4,5-B][1,4]苯并二氮杂卓-6-酮

LRRK2-IN-1 是一种选择性的LRRK2有效抑制剂，作用于 LRRK2 (G2019S) 和 LRRK2 (WT)，IC50值分别为 6 nM 和 13 nM。

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CAS：1234480-84-2

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生物活性化学信息储存和溶解度信息参考文献引用文献

产品描述

LRRK2-IN-1 is an effective and selective LRRK2 inhibitor.

体外活性

In HEK 293 cells stably expressing GFP-LRRK2[G2019S], LRRK2-IN-1 alters the cytoplasmic localization of LRRK2. In human-derived neuroblastoma SHSY5Y cells and mouse Swiss 3T3 cells, LRRK2-IN-1 induces a similar dose-dependent Ser910 and Ser935 dephosphorylation and loss of 14-3-3 binding to endogenous LRRK2. [1] In transgenic C. elegans expressing human R1441C- and G2019S-LRRK2, LRRK2-IN1 rescues the behavioral deficit characteristic of dopaminergic impairment. [2] In mouse fibroblasts, LRRK2-IN1 reduces cell motility. [3] In AsPC-1 and HCT116 cell lines, LRRK2-IN-1 shows anti-proliferative and pro-apoptotic properties, induces G1 and G2/M cell cycle arrest and inhibits DCLK1 mRNA and protein expression. [4]

体内活性

In wild type male C57BL/6 mice, LRRK2-IN-1 (100 mg/kg, i.p.) inhibits Ser910 and Ser935 dephosphorylation of LRRK2 in the kidney, while no effects in the brain. [1]

激酶实验

IC50 determination: Active GST-LRRK2 (1326-2527), GST-LRRK2 [G2019S] (1326-2527), GST-LRRK2 [A2016T] (1326-2527) and GST-LRRK2 [A2016T+G2019S] (1326-2527) enzyme is purified with glutathione sepharose from HEK293 cell lysate 36 h following transient transfection of the appropriate cDNA constructs. Peptide kinase assays, performed in duplicate, are set up in a total volume of 40 μL containing 0.5 μg LRRK2 kinase (which at approximately 10% purity gives a final concentration of 8 nM) in 50 mM Tris/HCl, pH 7.5, 0.1 mM EGTA, 10 mM MgCl2, 20 μM Nictide, 0.1 μM [γ-32P]ATP (~500 cpm/pmol) and the indicated concentrations of inhibitor dissolved in DMSO. After incubation for 15 min at 30 °C, reactions are terminated by spotting 35 μL of the reaction mix onto P81 phosphocellulose paper and immersion in 50 mM phosphoric acid. Samples are washed extensively and the incorporation of [γ-32P]ATP into Nictide is quantified by Cerenkov counting. IC50 values are calculated with GraphPad Prism using non-linear regression analysis.

细胞实验

Cells are seeded into a 96-well tissue culture plate in triplicate. The cells are cultured in the presence of LRRK2-IN-1 with DMSO as a vehicle at 0, 0.31, 0.63, 1, 2, and 5, 10, and 20 μM. 48 h post treatment, 10 μL of TACS MTT Reagent (RND Systems) is added to each well and the cells are incubated at 37°C until dark crystalline precipitate became visible in the cells. 100 μL of 266 mM NH4OH in DMSO is then added to the wells and placed on a plate shaker at low speed for 1 minute. After shaking, the plate is allowed to incubate for 10 minutes protected from light and the OD550 for each well is read using a microplate reader. The results are averaged and calculated as a percentage of the DMSO (vehicle) control +/- the standard error of the mean.(Only for Reference)

Cas No.

1234480-84-2

分子式

C31H38N8O3

分子量

570.698

别名

5,11-二氢-2-[[2-甲氧基-4-[[4-(4-甲基-1-哌嗪基)-1-哌啶基]羰基]苯基]氨基]-5,11-二甲基-6H-嘧啶并[4,5-B][1,4]苯并二氮杂卓-6-酮;LRRK2-IN-1

参考文献

[1]Weygant N, et al. Mol Cancer. 2014, 13, 103.[2]Caesar M, et al. Neurobiol Dis. 2013, 54, 280-288.[3]Yan R, Li J J, Zhou Y, et al. Inhibition of DCLK1 down-regulates PD-L1 expression through Hippo pathway in human pancreatic cancer[J]. Life Sciences. 2020, 241: 117150.[4]Yao C, et al. Hum Mol Genet. 2013, 22(2), 328-344.[5]Deng X, et al. Nat Chem Biol. 2011, 7(4), 203-205.

引用文献

[1]Yan R, Li J J, Zhou Y, et al. Inhibition of DCLK1 down-regulates PD-L1 expression through Hippo pathway in human pancreatic cancer. Life Sciences. 2020, 241: 117150

储存和溶解度

Ethanol:57 mg/mL (100 mM)
DMSO:57 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years

剂量换算 LRRK2-IN-1 1234480-84-2

对于各种应用，安全且有效的用药剂量是很有必要的了解更多

体内实验配液计算器

第一步：请输入动物实验的基本信息

剂量 mg/kg

每只动物体重 g

给药体积 ul

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO +

% +

% Tween 80 +

% ddH₂O

% DMSO +

重置计算

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

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已知质量的化合物在一定体积内形成的溶液的浓度

质量

浓度

体积

分子量

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制备已知体积和浓度溶液所需的化合物质量
将已知质量的化合物溶解到所需浓度所需的溶液体积
已知质量的化合物在一定体积内形成的溶液的浓度

浓度（起始）

体积（起始）

浓度（终点）

体积（终点）

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配液浓度

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输入化合物的化学式以计算其摩尔质量和元素组成
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分子结构式

总分子量

g/mol

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技术支持

在抑制剂处理说明中可以找到您可能遇到的问题的答案。主题包括如何准备储备溶液，如何存储产品以及基于细胞的测定和动物实验需要特别注意的问题。

Keywords

LRRK2 Leucine-rich repeat kinase 2 Inhibitor LRRK2 IN 1 Apoptosis LRRK2IN1 inhibit LRRK-2-IN-1 5,11-二氢-2-[[2-甲氧基-4-[[4-(4-甲基-1-哌嗪基)-1-哌啶基]羰基]苯基]氨基]-5,11-二甲基-6H-嘧啶并[4,5-B][1,4]苯并二氮杂卓-6-酮 1234480-84-2

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LRRK2-IN-1

5,11-二氢-2-[[2-甲氧基-4-[[4-(4-甲基-1-哌嗪基)-1-哌啶基]羰基]苯基]氨基]-5,11-二甲基-6H-嘧啶并[4,5-B][1,4]苯并二氮杂卓-6-酮

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