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Autophagy——LRRK2

Leucine-rich repeat kinase 2 (LRRK2) is a ubiquitously expressed member of the ROCO protein family. LRRK2 is a complex, multidomain protein containing kinase and GTPase enzymatic activities and multiple protein-protein interaction domains. LRRK2 is the genetic cause of both familial and idiopathic Parkinson's disease (PD), and it is associated with neuronal death, vesicle trafficking, mitochondrial dysfunction, and inflammation.

LRRK2 is a very large protein comprised of 2527 amino acids which has been determined to contain multiple functional domains, including armadillo (ARM), ankyrin-repeats (ANK), leucine-rich repeats (LRR), Ras of complex proteins (ROC), C-terminal of Roc (COR), MAPK-like kinase, and WD40 motifs. Mutations in LRRK2 represent a significant component of both sporadic and familial PD. Pathogenic mutations cluster in the enzymatic domains of LRRK2, and kinase activity seems to correlate with cytotoxicity, suggesting the possibility of kinase-based therapeutic strategies for LRRK2-associated PD. The best-characterized mutation to date, G2019S, leads to increased kinase activity, and mutations in the GTPase domain, such as R1441C and R1441G, have also been reported to influence kinase activity.

Autophagy——LRRK2(15)

Cat. No. Product Name CAS No. Purity Chemical Structure
KM9114 CZC-25146

CZC-25146是代谢稳定性的LRRK2抑制剂,对野生型LRRK2和G2019S LRRK2的IC50分别为4.76 nM和6.87 nM。

1191911-26-8 98%
KM17166 CZC-54252

CZC-54252 是一种有效的选择性 LRRK2 抑制剂,对野生型和 G2019S LRRK2IC50 分别为 1.28 nM 和 1.85 nM。CZC-54252 减弱由 G2019S LRRK2 诱导的人神经元损伤 ,EC50 约为 1 nM,具有神经保护活性。

1191911-27-9 99%
KM14528 GNE-7915

GNE-7915是高效选择性,可渗透大脑的LRRK2抑制剂,IC50值为9 nM。

1351761-44-8 99%
KM14529 GNE-7915 tosylate

GNE-7915 tosylate是高效选择性,可渗透大脑的LRRK2抑制剂,IC50值为9 nM。

2070015-00-6 99%
KM9037 GNE-9605

GNE 9605是一个高效,选择性和能脑渗透的LRRK2抑制剂,IC50为19 nM。

1536200-31-3 99%
KM11222 GNE0877

GNE0877是高活性、选择性、可通透脑屏障的LRRK2抑制剂,IC50为3 nM。

1374828-69-9 98%
KM8907 GSK2578215A

GSK2578215A 是 一种有效的选择性 LRRK2 抑制剂,作用于野生型 LRRK2 和 G2019S 突变型,IC50 值都约为 10 nM。

1285515-21-0 99%
KM9063 HG-10-102-01

HG-10-102-01是野生型LRRK2和突变型G2019S抑制剂,IC50分别为23.3 nM和3.2 nM。

1351758-81-0 99%
KM5680 IKK 16

IKK 16 是一种选择性的 IκB 激酶 (IKK) 抑制剂,作用于 IKK2IKK complexIKK1IC50 分别为 40 nM,70 nM 和 200 nM。IKK 16 还抑制富亮氨酸重复激酶 2 (LRRK 2),IC50 为 50 nM。

873225-46-8 99%
KM14931 JH-II-127

JH-II-127是一种高效的选择性, 脑渗透性LRRK2 抑制剂, 抑制LRRK2野生型, LRRK2-G2019S,和 LRRK2-A2016T, IC50 值分别为6.6 nM, 2.2 nM ,47.7 nM。

1700693-08-8 98%
KM6350 LRRK2 inhibitor 1

LRRK2 inhibitor 1 是有效,选择性的 LRRK2 抑制剂,IC50 为 6.8。

1802525-61-6 99%
KM7706 LRRK2-IN-1

LRRK2-IN-1 是一种有效的,选择性的 LRRK2 抑制剂,作用于 LRRK2 (G2019S) 和 LRRK2 (WT),IC50 值分别为 6 nM 和 13 nM。

1234480-84-2 99%
KM3304 MLi-2

MLi-2 是一种具有口服活性的,高选择性 LRRK2 抑制剂,IC50 为 0.76 nM。MLi-2 具有用于帕金森氏病的潜力。

1627091-47-7 99%
KM8052 PF-06447475

PF-06447475是高效,选择性,能透过血脑屏障的 LRRK2 抑制剂,IC50值为3 nM。

1527473-33-1 99%
KM6997 PFE-360

PFE-360 (PF-06685360) 是有效的、选择性的、能透过血脑屏障的、口服有效的 LRRK2 的抑制剂,体内测得的平均IC50 值为 2.3 nM。

1527475-61-1 98%
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