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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, CAS 1234480-84-2

规格	价格/CNY	货期
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

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选择批次

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

相关产品

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	在稳定表达GFP-LRRK2[G2019S]的HEK 293细胞中，LRRK2-IN-1改变了LRRK2的细胞质定位。在人源神经母细胞瘤SHSY5Y细胞和小鼠Swiss 3T3细胞中，LRRK2-IN-1引起剂量依赖性的Ser910和Ser935去磷酸化以及14-3-3蛋白与内源性LRRK2的结合丧失。[1] 在表达人类R1441C-和G2019S-LRRK2的转基因C. elegans中，LRRK2-IN1挽救了多巴胺能受损特有的行为缺陷。[2] 在小鼠成纤维细胞中，LRRK2-IN1降低了细胞移动性。[3] 在AsPC-1和HCT116细胞系中，LRRK2-IN-1显示出抗增殖和促凋亡属性，诱导G1和G2/M细胞周期阻滞，并抑制DCLK1 mRNA和蛋白表达。[4]
体内活性	在野生型雄性C57BL/6小鼠中，LRRK2-IN-1（100 mg/kg，i.p.）抑制肾脏中LRRK2的Ser910和Ser935去磷酸化，而在大脑中无效果。[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: 45 mg/mL (78.85 mM), Sonication is recommended.

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
Ethanol	100 mM	0.0175 mL	0.0876 mL	0.1752 mL	0.4381 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

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.

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.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

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。

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

给药体积

μL

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。

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