GNE0877
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
由于富亮氨酸重复激酶2 (LRRK2)作为帕金森病治疗潜在疾病修饰最有希望的靶点之一,其在神经科学研究领域引起显著兴趣.GNE-0877是高效选择性LRRK2抑制剂.
体外实验:GNE-0877具有显著增强的LRRK2胞内效应(3 nM)和在人肝微粒体及肝细胞中的低周转率,而无葡萄糖醛酸化作用.在0.1 μM GNE-0877的激酶选择性分析(188种激酶)中,仅对四种激酶表现出超过50%的抑制作用,表明GNE-0877是高选择性LRRK2抑制剂.而且,GNE-0877比TTK (Ki = 150 nM)的生化选择性指数高212倍[1].
体内试验:在表达G2019S帕金森病突变的人LRRK2蛋白的BAC转基因小鼠中评估GNE-0877在体内抑制LRRK2丝氨酸1292自磷酸化的能力.通过施予多种药物浓度发现,GNE-0877能以剂量依赖的方式显著抑制丝氨酸1292自磷酸化.
临床研究中:目前尚无临床数据.
参考文献:
[1] Estrada AA, Chan BK, Baker-Glenn C, Beresford A, Burdick DJ, Chambers M, Chen H, Dominguez SL, Dotson J, Drummond J, Flagella M, Fuji R, Gill A, Halladay J, Harris SF, Heffron TP, Kleinheinz T, Lee DW, Le Pichon CE, Liu X, Lyssikatos JP, Medhurst AD, Moffat JG, Nash K, Scearce-Levie K, Sheng Z, Shore DG, Wong S, Zhang S, Zhang X, Zhu H, Sweeney ZK. Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. J Med Chem. 2014 Feb 13;57(3):921-36.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 339.32 |
Cas No. | 1374828-69-9 |
Formula | C14H16F3N7 |
Solubility | ≥21 mg/mL in DMSO; ≥20 mg/mL in EtOH; insoluble in H2O |
Chemical Name | 2-methyl-2-(3-methyl-4-((4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)-1H-pyrazol-1-yl)propanenitrile |
SDF | Download SDF |
Canonical SMILES | FC(F)(C1=CN=C(N=C1NC)NC2=CN(C(C)(C#N)C)N=C2C)F |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Description | GNE-0877是富亮氨酸重复激酶2 (LRRK2)的高效选择性抑制剂,Ki值为0.7 nM. | |||||
靶点 | LRRK2 | |||||
IC50 | Ki=0.7 nM |
质量控制和MSDS
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