1. Autophagy
  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 Related Products (13):

Cat. No. Product Name Effect Purity
  • HY-18163
    GNE-7915 Inhibitor 98.77%
    GNE-7915 is a potent, selective and brain-penetrant inhibitor of LRRK2 with an IC50 of 9 nM.
  • HY-10875
    LRRK2-IN-1 Inhibitor 99.38%
    LRRK2-IN-1 is a cell-permeable, ATP competitive, potent, and selective LRRK2 inhibitor.
  • HY-12477
    PF-06447475 Inhibitor 99.62%
    PF-06447475 is a highly potent, selective and brain penetrant LRRK2 inhibitor with an IC50 of 3 nM.
  • HY-13488
    HG-10-102-01 Inhibitor 99.54%
    HG-10-102-01 is a potent and selective inhibitor of wild-type LRRK2(IC50=23.3 nM) and the G2019S mutant(IC50=3.2 nM) IC50 Value: 23.3 nM (WT LRRK2); 3.2 nM (LRRK2 G2019S) [1] Target: LRRK2 HG-10-102-01 maintains the ability to potently inhibit the biochemical activity of wild-type and G2019S mutant LRRK2.
  • HY-13237
    GSK2578215A Inhibitor
    GSK2578215A is a potent and highly selective LRRK2 inhibitor; exhibits IC50s of around 10 nM against both wild-type LRRK2 and the G2019S mutant.
  • HY-100411
    MLi-2 Inhibitor 98.56%
    MLi-2 is an a potent, highly selective, orally available, brain penetrant inhibitor of LRRK2 with an IC50 of 0.76 nM.
  • HY-12282
    GNE-9605 Inhibitor 99.34%
    GNE-9605 is a highly potent, selective, and brain-penetrant LRRK2 inhibitor with IC50 of 19 nM.
  • HY-15800A
    CZC-25146 Inhibitor
    CZC-25146 is a potent, selective and metabolically stable LRRK2 inhibitor with IC50 of 4.76 nM/6.87 nM for wild type LRRK2 and G2019S LRRK2 respectively.
  • HY-16936
    JH-II-127 Inhibitor
    JH-II-127 is a highly potent, selective, and brain penetrant LRRK2 inhibitor, with IC50 of 6.6 nM, 2.2 nM ,47.7 nM for LRRK2-wild-type, LRRK2-G2019S, LRRK2-A2016T.
  • HY-B0792
    CZC-54252 Inhibitor
    CZC-54252 is a potent inhibitor of LRRK2 with IC50s of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2 respectively.
  • HY-18163A
    GNE-7915 tosylate Inhibitor
    GNE-7915 tosylate is a potent, selective and brain-penetrant inhibitor of LRRK2 with an IC50 of 9 nM.
  • HY-15796
    GNE0877 Inhibitor
    GNE0877 is a highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitor with an IC50 of 3 nM.
  • HY-15800
    CZC-25146 hydrochloride Inhibitor
    CZC-25146 Hcl is a potent, selective and metabolically stable LRRK2 inhibitor with IC50 of 4.76 nM/6.87 nM for wild type LRRK2 and G2019S LRRK2 respectively.