LRRK2-IN-1
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.
LRRK2-IN-1是有效的LRRK2选择性抑制剂,其IC50值为13 nM[1]。
LRRK2(富亮氨酸重复激酶2)也被称为dardarin。LRRK2属于富亮氨酸重复激酶家族。LRRK2大多分布于细胞质中,但也可以结合到线粒体外膜。LRRK2与parkin蛋白的C端R2 RING指结构域相互作用。而Parkin与LRRK2的COR结构域相互作用。LRRK2突变可以诱导神经母细胞瘤细胞凋亡。LRRK2突变体的表达与常染色体显性遗传的帕金森氏病密切相关。LRRK2 Gly2019Ser突变是家族性帕金森氏病的常见成因。即使LRRK2突变数量少,Gly2019Ser也足以引起帕金森氏病。全基因组关联研究表明,LRRK2还与克罗恩氏病相关。
在稳定表达带有GFP标签的野生型或突变体LRRK2的HEK293细胞中,LRRK2-IN-1呈剂量依赖性地抑制野生型以及G2019S LRRK2的活性,IC50值分别为0.17和0.04 μM[2]。在含0.1 mM ATP的体外酶实验中,LRRK2-IN-1抑制野生型和突变体G2019S LRRK2,IC50值分别为13 nM和6 nM。LRRK2-IN-1与ATP竞争。与其它442种不同的激酶相比,LRRK2-IN-1具有选择性,对LRRK1没有抑制作用。LRRK2-IN-1诱导淋巴母细胞中的内源性LRRK2磷酸化。在小鼠肾脏中,100 mg/kg的LRRK2-IN-1也可以诱导LRRK2 Ser910/Ser935去磷酸化[1]。
参考文献:
[1]. Deng X, Dzamko N, Prescott A, Davies P, Liu Q, Yang Q, Lee JD, Patricelli MP, Nomanbhoy TK, Alessi DR et al: Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2. Nat Chem Biol, 7(4):203-205.
[2]. Hermanson SB, Carlson CB, Riddle SM, Zhao J, Vogel KW, Nichols RJ, Bi K: Screening for novel LRRK2 inhibitors using a high-throughput TR-FRET cellular assay for LRRK2 Ser935 phosphorylation. PLoS One, 7(8):e43580.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 570.7 |
Cas No. | 1234480-84-2 |
Formula | C31H38N8O3 |
Synonyms | LRRK 2-IN-1 |
Solubility | ≥28.55 mg/mL in DMSO; insoluble in H2O; ≥57.2 mg/mL in EtOH |
Chemical Name | 2-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]anilino]-5,11-dimethylpyrimido[4,5-b][1,4]benzodiazepin-6-one |
SDF | Download SDF |
Canonical SMILES | CN1CCN(CC1)C2CCN(CC2)C(=O)C3=CC(=C(C=C3)NC4=NC=C5C(=N4)N(C6=CC=CC=C6C(=O)N5C)C)OC |
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 | LRRK2-IN-1是有效的富亮氨酸重复激酶2(LRRK2)选择性抑制剂,对野生型LRRK2和G2019S突变LRRK2的IC50值分别为13 nM和6 nM。 | |||||
靶点 | wild-type LRRK2 | G2019S mutant LRRK2 | ||||
IC50 | 13 nM | 6 nM |
质量控制和MSDS
- 批次: