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Submit ReviewLRRK2-IN-1
说明： Potent and selective LRRK2 inhibitor
化学名： 5,11-Dihydro-2-[[2-methoxy-4-[[4-(4-methyl-1-piperazinyl)-1-piperidinyl]carbonyl]phenyl]amino]-5,11-dimethyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one
纯度： ≥98% (HPLC)
生物活性 for LRRK2-IN-1
LRRK2-IN-1 is a potent and selective inhibitor of leucine-rich repeat kinase 2 (LRRK2). Inhibits both G2019S mutant and wild-type LRRK2 kinase activity (IC50 values are 6 and 13 nM respectively). Causes dephosphorylation, ubiquitination and degradation of LRRK2. Inhibits IFN-γ-induced monocyte maturation in vitro.
许可信息
Sold under license from the Dana-Farber Cancer Institute.
化合物库 for LRRK2-IN-1
LRRK2-IN-1 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for LRRK2-IN-1
| 分子量 | 570.69 |
| 公式 | C31H38N8O3 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1234480-84-2 |
| PubChem ID | 46843906 |
| InChI Key | IWMCPJZTADUIFX-UHFFFAOYSA-N |
| Smiles | O=C2C3=C(C=CC=C3)N(C)C1=NC(NC4=C(OC)C=C(C(N5CCC(N6CCN(C)CC6)CC5)=O)C=C4)=NC=C1N2C |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for LRRK2-IN-1
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 57.01 | 100 | |
| ethanol | 57.01 | 100 |
制备储备液 for LRRK2-IN-1
以下数据基于产品分子量 570.69。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.75 mL | 8.76 mL | 17.52 mL |
| 5 mM | 0.35 mL | 1.75 mL | 3.5 mL |
| 10 mM | 0.18 mL | 0.88 mL | 1.75 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.35 mL |
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产品说明书 for LRRK2-IN-1
参考文献 for LRRK2-IN-1
参考文献是支持产品生物活性的出版物。
Deng et al (2011) Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2. Nat.Chem.Biol. 7 203 PMID: 21378983
Zhao et al (2015) LRRK2 Dephosphorylation increases its ubiquitination. Biochem.J. 469 107 PMID: 25939886
Thévenet et al (2011) Regulation of LRRK2 expression points to a functional role in human monocyte maturation. PLoS One 6 e21519 PMID: 21738687
If you know of a relevant reference for LRRK2-IN-1, please let us know.
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关键词: LRRK2-IN-1, LRRK2-IN-1 supplier, parkinsons, disease, lrrk2, leucine-rich, repeat, kinase, 2, dardarin, parkinson's, LRRK2, 4273, Tocris Bioscience
7 篇 LRRK2-IN-1 的引用文献
引用文献是使用了 Tocris 产品的出版物。 LRRK2-IN-1 的部分引用包括：
Chia et al (2014) Phosphorylation of LRRK2 by casein kinase 1α regulates trans-Golgi clustering via differential interaction with ARHGEF7. BMC Cancer 5 5827 PMID: 25500533
Elisa et al (2019) Leucine-rich repeat kinase 2 phosphorylation on synapsin I regulates glutamate release at pre-synaptic sites. J Neurochem 150 264-281 PMID: 31148170
Chen et al (2017) Phosphorylation of amyloid precursor protein by mutant LRRK2 promotes AICD activity and neurotoxicity in Parkinson's disease. Sci Signal 10 PMID: 28720718
Saez-Atienzar et al (2014) The LRRK2 inhibitor GSK2578215A induces protective autophagy in SH-SY5Y cells: involvement of Drp-1-mediated mitochondrial fission and mitochondrial-derived ROS signaling. Cell Death Dis. 5 e1368 PMID: 25118928
Reynolds et al (2014) LRRK2 kinase activity and biology are not uniformly predicted by its autophosphorylation and cellular phosphorylation site status. Front Mol Neurosci 7 54 PMID: 25009464
Chen et al (2017) LRRK2 interacts with ATM and regulates Mdm2-p53 cell proliferation axis in response to genotoxic stress. Hum Mol Genet 26 4494 PMID: 28973420
Bae et al (2018) Brain injury induces HIF-1α-dependent transcriptional activation of LRRK2 that exacerbates brain damage. Cell Death Dis 9 1125 PMID: 30420654
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Parkinson's Disease Poster
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.