LRRK2
Leucine-rich repeat kinase 2 (LRRK2) is a complex, scaffolding protein containing ankyrin, leucine-rich and WD40 repeats, and a catalytic core with Ras-Of-Complex (ROC) GTPase and serine-threonine kinase activities. LRRK2 belongs to the family of ROCOs, multidomain proteins identified in a wide range of species, from prokaryotes to eukaryotes including humans. ROCO proteins possess a ROC domain invariably followed by a C-terminus Of ROC (COR) domain likely involved in protein dimerization. ROCO proteins, including LRRK2, have been implicated in a variety of fundamental biological processes converging in cytoskeletal and vesicle dynamics. Nominated LRRK2 substrates are clustered within three major biological categories – (1) cytoskeleton dynamics, (2) vesicle-related processes and (3) protein transcription/translation - and there are robust functional indications linking LRRK2 with these processes. With regard to cytoskeleton dynamics, LRRK2 has been reported to phosphorylate a number of cytoskeletal-related proteins including tau, the tau kinase MARK1, tubulins, ARHGEF7, ezrin-radixin-moesin (ERM) and the Drosophila microtubule (MT)-binding protein Futsch.
References
1.Taymans JM,et al. Curr Neuropharmacol. 2016;14(3):214–225.
References
1.Taymans JM,et al. Curr Neuropharmacol. 2016;14(3):214–225.
Autophagy
LRRK2
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LRRK2-IN-7
产品货号 : M36503
cas no: 2307277-93-4
LRRK2-IN-7 是一种有效的、选择性的、CNS 渗透性 LRRK2 激酶抑制剂,IC50 为 0.9 nM。LRRK2-IN-7 的选择性是其他激酶、离子通道和 CYP 酶的 1000 倍以上。 -
EB-42486
产品货号 : M28245
cas no: 2390475-81-5
EB-42486 是一种有效且高度选择性的 G2019S-LRRK2 抑制剂,IC50 < 0.2 nM。 -
CZC-54252 hydrochloride
产品货号 : M28212
cas no: 1784253-05-9
CZC-54252 Hydrochloride 是 LRRK2 的选择性抑制剂,对野生型和 G2019S LRRK2 的 IC50 分别为 1.85 nM 和 1.28 nM。 -
PF-06454589
产品货号 : M20924
cas no: 1527473-30-8
PF-06454589 是 LRRK2 的有效抑制剂。 -
HG-10-102-01
产品货号 : M20640
cas no: 1351758-81-0
HG-10-102-01 是富含亮氨酸重复激酶 2(LRRK2,IC50 为 20.3 nM)的抑制剂。