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 (18):

目录号 产品名 作用方式 纯度
  • HY-100411
    MLi-2 Inhibitor 99.74%
    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。
  • HY-13687
    IKK 16 Inhibitor 99.09%
    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。
  • HY-120085
    PFE-360 Inhibitor 98.94%
    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。
  • HY-12477
    PF-06447475 Inhibitor 99.88%
    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。
  • HY-18163
    GNE-7915 Inhibitor 99.79%
    GNE-7915是高效选择性,可渗透大脑的LRRK2抑制剂,IC50值为9 nM。
  • HY-10875
    LRRK2-IN-1 Inhibitor 99.19%
    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。
  • HY-15796
    GNE0877 Inhibitor 98.89%
    GNE0877是高活性、选择性、可通透脑屏障的LRRK2抑制剂,IC50为3 nM。
  • HY-13488
    HG-10-102-01 Inhibitor 99.57%
    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。
  • HY-13237
    GSK2578215A Inhibitor 99.79%
    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。
  • 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-16936
    JH-II-127 Inhibitor 98.02%
    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。
  • 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-111493
    LRRK2 inhibitor 1 Inhibitor 99.72%
    LRRK2 inhibitor 1 是有效,选择性的 LRRK2 抑制剂,IC50 为 6.8。
  • 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-13687A
    IKK 16 hydrochloride Inhibitor
    IKK 16 hydrochloride 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。
  • 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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