2. Signaling Pathways
  3. Autophagy
  4. LRRK2

LRRK2

Leucine-rich repeat kinase 2

LRRK2

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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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-100411
    MLi-2
    		Inhibitor 99.80%
    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.
    MLi-2
  • HY-13687
    IKK 16
    		Inhibitor 99.88%
    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.
    IKK 16
  • HY-10875
    LRRK2-IN-1
    		Inhibitor 99.42%
    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.
    LRRK2-IN-1
  • HY-12477
    PF-06447475
    		Inhibitor 99.94%
    PF-06447475 is a highly potent, selective and brain penetrant LRRK2 inhibitor with an IC50 of 3 nM.
    PF-06447475
  • HY-15796
    GNE0877
    		Inhibitor 99.81%
    GNE0877 is a highly selective, orally active and brain-penetrant LRRK2 inhibitor with an IC50 of 3 nM and a Ki of 0.7 nM. GNE0877 can be used for the research of neuroscience.
    GNE0877
  • HY-168041
    LRRK2-IN-15
    		Inhibitor
    LRRK2-IN-15 is an LRRK2 inhibitor. The IC50 value for PBMC cells is 5 nM, and the IC50 value for BCRP is 1.5 μM. LRRK2-IN-15 can be used for research on Parkinson's disease.
    LRRK2-IN-15
  • HY-162699
    LY2023-001
    		Inhibitor
    LY2023-001 is a potent G2019S LRRK2 inhibitor with an IC50 of 12.9 nM. LY2023-001 formed stable hydrogen bonds with Glu1948, and Ala1950 in the G2019S LRRK2 protein.
    LY2023-001
  • HY-P10636
    Nictide
    Nictide is a peptide substrate of LRRK2 (leucine-rich repeat protein kinase-2). Nictide can be phosphorylated by the activated LRRK2[G2019S] with a Km of 10 μM.
    Nictide
  • HY-148030
    XL01126
    		Inhibitor 99.81%
    XL01126 is a potent LRRK2 PROTAC (DC50: 14 nM (G2019S LRRK2) and 32 nM (WT LRRK2)) composed of the VHL ligand VH 101, thiol (HY-47851, blue part) and the LRRK2 inhibitor HG-10-102-01 (HY-13488, red part). XL01126 crosses the blood-brain barrier and is used as a degradation probe in Parkinson's disease research. XL01126 can be used to study the non-catalytic and framework functions of LRRK2.
    XL01126
  • HY-18163
    GNE-7915
    		Inhibitor 99.82%
    GNE-7915 is a potent, selective and brain-penetrant inhibitor of LRRK2 with an IC50 of 9 nM.
    GNE-7915
  • HY-13237
    GSK2578215A
    		Inhibitor 99.78%
    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.
    GSK2578215A
  • HY-120085
    PFE-360
    		Inhibitor 99.48%
    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.
    PFE-360
  • HY-13488
    HG-10-102-01
    		Inhibitor 99.55%
    HG-10-102-01 is a highly potent, selective, and brain-penetrable LRRK2 inhibitor, with IC50 values of 20.3 and 3.2 nM against wild-type LRRK2 and LRRK2[G2019S], respectively. HG-10-102-01 also inhibits MNK2 and MLK1, with IC50 values of 0.6 and 2.1 μM. HG-10-102-01 can be used for Parkinson's disease (PD) research.
    HG-10-102-01
  • HY-13687A
    IKK 16 hydrochloride
    		Inhibitor 99.95%
    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.
    IKK 16 hydrochloride
  • HY-15800A
    CZC-25146
    		Inhibitor 99.10%
    CZC-25146 is a potent and orally active LRRK2 inhibitor with IC50 values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. CZC-25146 prevents mutant LRRK2-induced injury of neurons in vitro. CZC-25146 exhibits relatively favorable pharmacokinetic properties in mice. CZC-25146 can increase normal α-1-antitrypsin (AAT) secretion and reduce inflammatory cytokines. CZC-25146 can be used to research Parkinson's disease and liver diseases.
    CZC-25146
  • HY-40294
    Indazole
    		Inhibitor 99.72%
    Indazole, also called isoindazole, a heterocyclic aromatic organic compound. Its derivatives display a broad variety of biological activities including anti-inflammatory, antibacterial, anti-HIV, antiarrhythmic, antifungal and antitumour properties. Indazole and its derivatives can be used for research of cancer, neurological disorders, cardiovascular diseases, gastrointestinal diseases.
    Indazole
  • HY-112855
    PF-06454589
    		Inhibitor 99.91%
    PF-06447475 is a highly potent, selective, brain penetrant LRRK2 kinase inhibitor with IC50 values of 3 nM and 11 nM for WT LRRK and G2019S LRRK2, respectively. PF-06447475 can be used for parkinson's disease (PD) research.
    PF-06454589
  • HY-B0792
    CZC-54252
    		Inhibitor 99.38%
    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.
    CZC-54252
  • HY-12282
    GNE-9605
    		Inhibitor 99.72%
    GNE-9605 is a potent, orally active, selective Leucine-rich repeat kinase 2 (LRRK2) inhibitor with an IC50 value of 18.7 nM. GNE-9605 inhibits LRRK2 Ser1292 autophosphorylation. GNE-9605 can be used in research of Parkinson's disease (PD) .
    GNE-9605
  • HY-112809
    GSK2646264
    		Inhibitor 98.39%
    GSK2646264 (Compound 44) is a potent and selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.1. GSK2646264 also inhibits other kinases with pIC50 values of 5.4, 5.4, 5.3, 5, 4.5, <4.6 and <4.3 against LCK, LRRK2, GSK3β, JAK2, VEGFR2/KDR/Flk-1, Aurora B and Aurora A, respectively. GSK2646264 is penetrable into the epidermis and dermis of the skin.
    GSK2646264
Cat. No. Product Name / Synonyms Application Reactivity