1. Signaling Pathways
  2. Autophagy
  3. LRRK2

LRRK2 (富亮氨酸重复激酶2)

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.

LRRK2 相关产品 (6):

Cat. No. Product Name Effect Purity
  • HY-12282
    GNE-9605 Inhibitor 99.72%
    GNE 9605是一个高效,选择性和能脑渗透的LRRK2抑制剂,IC50为19 nM。
  • HY-B0792
    CZC-54252 Inhibitor 99.18%
    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。
  • HY-15800A
    CZC-25146 Inhibitor 98.64%
    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。
  • HY-18163A
    GNE-7915 tosylate Inhibitor 99.62%
    GNE-7915 tosylate是高效选择性,可渗透大脑的LRRK2抑制剂,IC50值为9 nM。
  • HY-B0792A
    CZC-54252 hydrochloride Inhibitor
    CZC-54252 hydrochloride 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 hydrochloride 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。
  • HY-15800
    CZC-25146 hydrochloride Inhibitor
    CZC-25146盐酸盐是代谢稳定的LRRK2选择性抑制剂,对野生型LRRK2和G2019S LRRK2的IC50分别为4.76 nM和6.87 nM。
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