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  2. LRRK2

LRRK2

Leucine-rich repeat kinase 2 (LRRK2) is an enzyme that in humans is encoded by the PARK8 gene. LRRK2 is a member of the leucine-rich repeat kinase family. Variants of this gene are associated with an increased risk of Parkinson's disease (PD)and also Crohn's disease (CD).

Leucine-rich repeat kinase 2 (LRRK2) is the gene responsible for autosomal-dominant PD, PARK8, which is originally defined by linkage analysis of a Japanese family. LRRK2 is a complex kinase consisting of LRR, ROC, COR, kinase, and WD40 domains. LRRK2 plays a key role in axonal extension, autophagy, proliferation, and survival of neurons. In addition to neurons, LRRK2 is highly expressed in immune cells such as B cells, macrophages, and microglia. Several studies have demonstrated that LRRK2 is related to inflammatory responses of microglia that could be involved in the development and progression of neurodegeneration.

LRRK2 is a large, multidomain protein containing two catalytic domains: a Ras of complex proteins (Roc) G-domain and a kinase domain. Leucine-rich repeat kinase 2 (LRRK2) represents a promising drug target for treatment and prevention of Parkinson’s disease (PD), because mutations in LRRK2 are the most common cause of Mendelian forms of the disease. PD-associated LRRK2 variants show decreased GTPase and increased kinase activity.

LRRK2 相关产品 (13):

Cat. No. Product Name Effect Purity
  • HY-10875
    LRRK2-IN-1 Inhibitor 99.38%
    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-18163
    GNE-7915 Inhibitor 98.77%
    GNE-7915是高效选择性,可渗透大脑的LRRK2抑制剂,IC50值为9 nM。
  • HY-12477
    PF-06447475 Inhibitor 99.62%
    PF-06447475是高效选择性有闹渗透性的LRRK2抑制剂,IC50值为3 nM。
  • HY-13488
    HG-10-102-01 Inhibitor 99.54%
    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 99.86%
    GSK2578215A是LRRK2高效选择性抑制剂,对野生型LRRK2和突变型G2019S的IC50值约为10nM。
  • HY-15800A
    CZC-25146 Inhibitor
    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-16936
    JH-II-127 Inhibitor
    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-12282
    GNE-9605 Inhibitor 99.26%
    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-100411
    MLi-2 Inhibitor 99.66%
    MLi-2是高效选择的,具有口服活性,可渗透大脑的LRRK2抑制剂。IC50值为0.76 nM。
  • HY-B0792
    CZC-54252 Inhibitor 99.26%
    CZC-54252是LRRK2高效抑制剂,对野生型LRRK2和突变型G2019S LRRK2的IC50值分别为1.28和1.85nM。
  • HY-18163A
    GNE-7915 tosylate Inhibitor
    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-15796
    GNE0877 Inhibitor
    GNE0877是高活性、选择性、可通透脑屏障的LRRK2抑制剂,IC50为3 nM。
  • 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。