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LRRK2-IN-1

LRRK2-IN-1

产品编号 T2246   CAS 1234480-84-2
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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LRRK2-IN-1 Chemical Structure
LRRK2-IN-1, CAS 1234480-84-2
规格 价格/CNY 货期 数量
1 mg ¥ 219 现货
5 mg ¥ 489 现货
10 mg ¥ 788 现货
25 mg ¥ 1,570 现货
50 mg ¥ 2,990 现货
100 mg ¥ 4,390 现货
500 mg ¥ 9,490 现货
1 mL * 10 mM (in DMSO) ¥ 718 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
MG-132限时半价
重组蛋白限时优惠
产品目录号及名称: LRRK2-IN-1 (T2246)
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纯度: 98.44%
纯度: 98.44%
纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 LRRK2-IN-1 is an effective and selective LRRK2 inhibitor.
靶点活性 LRRK2 (WT):13 nM, DCLK2:45 nM, LRRK2 (G2019S):6 nM
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)
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
分子量 570.69
分子式 C31H38N8O3
CAS No. 1234480-84-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 57 mg/mL (100 mM)

DMSO: 57 mg/mL (100 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 1.7523 mL 8.7613 mL 17.5226 mL 43.8066 mL
5 mM 0.3505 mL 1.7523 mL 3.5045 mL 8.7613 mL
10 mM 0.1752 mL 0.8761 mL 1.7523 mL 4.3807 mL
20 mM 0.0876 mL 0.4381 mL 0.8761 mL 2.1903 mL
50 mM 0.035 mL 0.1752 mL 0.3505 mL 0.8761 mL
100 mM 0.0175 mL 0.0876 mL 0.1752 mL 0.4381 mL

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TargetMol Library Books参考文献

1. Deng X, et al. Nat Chem Biol. 2011, 7(4), 203-205. 2. Yao C, et al. Hum Mol Genet. 2013, 22(2), 328-344. 3. Caesar M, et al. Neurobiol Dis. 2013, 54, 280-288. 4. Weygant N, et al. Mol Cancer. 2014, 13, 103. 5. 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.

TargetMol Library Books文献引用

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 2. Wan J, He Z, Peng R, et al.Injectable photocrosslinking spherical hydrogel-encapsulated targeting peptide-modified engineered exosomes for osteoarthritis therapy.Journal of Nanobiotechnology.2023, 21(1): 1-21.
Nirogacestat Trigonelline Asiatic acid Perifosine Trolox Diffractaic Acid Iberdomide Doxorubicin hydrochloride

相关化合物库

该产品包含在如下化合物库中:
神经退行性疾病化合物库 抑制剂库 激酶抑制剂库 抗癌化合物库 NO PAINS 化合物库 细胞周期化合物库 抗衰老化合物库 抗帕金森病化合物库 经典已知活性库 抗乳腺癌化合物库

TargetMol Calculator剂量换算

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 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 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

LRRK2-IN-1 1234480-84-2 Apoptosis Autophagy Cell Cycle/Checkpoint LRRK2 CDK Leucine-rich repeat kinase 2 Inhibitor LRRK2 IN 1 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 inhibitor

 

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