1. Signaling Pathways
  2. Autophagy
  3. LRRK2

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.

LRRK2 Related Products (18):

Cat. No. Product Name Effect Purity
  • HY-100411
    MLi-2 Inhibitor 99.74%
    MLi-2 is an orally active and highly selective LRRK2 inhibitor with an IC50 of 0.76 nM. MLi-2 has the potential for Parkinson’s disease.
  • HY-13687
    IKK 16 Inhibitor 99.09%
    IKK 16 is a selective IκB kinase (IKK) inhibitor for IKK2, IKK complex and IKK1 with IC50s of 40 nM, 70 nM and 200 nM, respectively. IKK16 also inhibits leucine-rich repeat kinase-2 (LRRK2) with an IC50 of 50 nM.
  • HY-12477
    PF-06447475 Inhibitor 99.88%
    PF-06447475 is a highly potent, selective and brain penetrant LRRK2 inhibitor with an IC50 of 3 nM.
  • HY-120085
    PFE-360 Inhibitor 98.94%
    PFE-360 (PF-06685360) is a potent, selective, brain penetrated and orally active leucine-rich repeat kinase 2 (LRRK2) inhibitor with a mean IC50 of 2.3 nM in vivo.
  • HY-18163
    GNE-7915 Inhibitor 99.79%
    GNE-7915 is a potent, selective and brain-penetrant inhibitor of LRRK2 with an IC50 of 9 nM.
  • HY-B0792A
    CZC-54252 hydrochloride Inhibitor
    CZC-54252 hydrochloride is a potent and selective LRRK2 inhibitor with IC50s of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2, respectively. G2019S LRRK2-induced human neuronal injury is attenuated by CZC-54252 hydrochloride with an EC50 of ~1 nM.CZC-54252 hydrochloride has a neuroprotective activity.
  • HY-15796
    GNE0877 Inhibitor 98.07%
    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-10875
    LRRK2-IN-1 Inhibitor 99.19%
    LRRK2-IN-1 is a potent and selective LRRK2 inhibitor with IC50 of 6 nM and 13 nM for LRRK2 (G2019S) and LRRK2 (WT), respectively.
  • HY-13237
    GSK2578215A Inhibitor 99.79%
    GSK2578215A is a potent and highly selective LRRK2 inhibitor, which exhibits IC50s of around 10 nM against both wild-type LRRK2 and the G2019S mutant.
  • HY-13488
    HG-10-102-01 Inhibitor 99.57%
    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-12282
    GNE-9605 Inhibitor 99.72%
    GNE-9605 is a highly potent, selective, and brain-penetrant LRRK2 inhibitor with IC50 of 19 nM.
  • HY-16936
    JH-II-127 Inhibitor 98.02%
    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 99.18%
    CZC-54252 is a potent and selective LRRK2 inhibitor with IC50s of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2, respectively. CZC-54252 attenuates G2019S LRRK2-induced human neuronal injury with an EC50 of ~1 nM. CZC-54252 has a neuroprotective activity.
  • HY-15800A
    CZC-25146 Inhibitor 98.64%
    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-111493
    LRRK2 inhibitor 1 Inhibitor 99.72%
    LRRK2 inhibitor 1 is a potent, selective and oral LRRK2 inhibitor with an pIC50 of 6.8.
  • HY-18163A
    GNE-7915 tosylate Inhibitor 99.62%
    GNE-7915 tosylate is a potent, selective and brain-penetrant inhibitor of LRRK2 with an IC50 of 9 nM.
  • HY-13687A
    IKK 16 hydrochloride Inhibitor
    IKK 16 hydrochloride is a selective IκB kinase (IKK) inhibitor for IKK2, IKK complex and IKK1 with IC50s of 40 nM, 70 nM and 200 nM, respectively. IKK16 also inhibits leucine-rich repeat kinase-2 (LRRK2) with an IC50 of 50 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.
Isoform Specific Products

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