LRRK2-IN-1
货号:
18094-1mg 基本售价:
350.0 元 规格:
1 mg
产品信息
概述货号 | 18094-1mg |
描述 | Leucine-rich repeat kinase 2 (LRRK2) is an enzyme that interacts with parkin, a ligase that is part of the ubiquitin-proteasome system that mediates the targeting of proteins for degradation. Loss of function of the parkin protein leads to dopaminergic cell death. The development of Parkinsons disease has been strongly associated with mutations in the LRRK2 gene that lead to increased kinase activity. LRRK2-IN-1 is a potent inhibitor of LRRK2 that inhibits both wild-type and G2019S mutant LRRK2 (IC50s = 13 and 6 nM, respectively).1 It is selective for LRRK2 over a large panel of other kinases. LRRK2-IN-1 treatment causes dephosphorylation of LRRK2, leading to its dissociation from 14-3-3 proteins, ubiquitination, and degradation.1,2 Inhibitors of LRRK2, including LRRK2-IN-1, stimulate macroautophagy in H4 neuroglioma cells.3 |
别名 | Leucine-rich repeat kinase 2 IN-1; |
性能供应商 | Cayman |
应用文献 |
1.Deng, X.,Dzamko, N.,Prescott, A., et al. Characterization of a selective inhibitor of the Parkinson’s disease kinase LRRK2. Nature Chemical Biology 7(4), 203-205 (2011). 2.Zhao, J.,Molitor, T.P.,Langston, J.W., et al. LRRK2 dephosphorylation increases its ubiquitination. Biochemistry Journal 469, 107-120 (2015). 3.Manzoni, C.,Mamais, A.,Dihanich, S., et al. Inhibition of LRRK2 kinase activity stimulates macroautophagy. Biochem.Biophys.Acta. 1833, 2900-2910 (2013).
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运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥95% |
计算分子量 | 570.7 |
分子式 | C31H38N8O3 |
CAS号 | 1234480-84-2 |
稳定性 | ≥ 2 years |
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