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-16936
    JH-II-127
    		Inhibitor ≥98.0%
    JH-II-127 is an orally active, highly potent, selective and brain-permeable LRRK2 inhibitor, with IC50s of 6, 2 and 48 nM for wild-type LRRK2 and LRRK2-G2019S and mutant LRRK2-A2016T. JH-II-127 inhibits Ser935 phosphorylation in all tissues of mice, including the brain. JH-II-127 can be used in the study of parkinson's syndrome.
    JH-II-127
  • HY-142647
    EB-42486
    		Inhibitor 99.62%
    EB-42486 is a novel, potent, and highly selective G2019S-LRRK2 inhibitor (IC50 < 0.2 nM).
    EB-42486
  • HY-163064
    CC-3240
    		Degrader 98.23%
    CC-3240 (compound 13) is a molecular glue degrader of CaMKK2 based on CC-8977, with the IC50 of 9 nM.
    CC-3240
  • HY-152107
    LRRK2-IN-7
    		Inhibitor 98.04%
    LRRK2-IN-7 is a potent, selective, and CNS-penetrant LRRK2 kinase inhibitor with an IC50 of 0.9 nM. LRRK2-IN-7 shows >1000-fold selectivity over other kinases, ion channels, and CYP enzymes.
    LRRK2-IN-7
  • HY-111493
    LRRK2 inhibitor 1
    		Inhibitor 99.93%
    LRRK2 inhibitor 1 is a potent, selective and oral LRRK2 inhibitor with an pIC50 of 6.8.
    LRRK2 inhibitor 1
  • HY-156429
    MK-1468
    		Inhibitor 98.01%
    MK-1468 is a high selective and brain-penetrant inhibitor of LRRK2 with an IC50 of 0.8 nM. MK-1468 can be used in study Parkinson’s disease.
    MK-1468
  • HY-18163A
    GNE-7915 tosylate
    		Inhibitor 99.69%
    GNE-7915 tosylate is a potent, selective and brain-penetrant inhibitor of LRRK2 with an IC50 of 9 nM.
    GNE-7915 tosylate
  • HY-145317
    LRRK2-IN-2
    		Inhibitor
    LRRK2-IN-2 (compoubd 22) is a potent, selective, orally active and brain-penetrant inhibitor LRRK2, with IC50 of <0.6 nM. LRRK2-IN-2 can be used for the research of Parkinson's disease.
    LRRK2-IN-2
  • HY-153058
    LRRK2-IN-8
    		Inhibitor
    LRRK2-IN-8 is a LRRK2 inhibitor. LRRK2-IN-8 inhibits LRRK2 (wt) and LRRK2 (G2019) with IC50s lower than 10 nM, and inhibits TYK2 and NUAK1 with IC50s of 10-100 nM.
    LRRK2-IN-8
  • HY-145318
    LRRK2-IN-3
    		Inhibitor
    LRRK2-IN-3 (compoubd 24) is a potent, selective, orally active and brain-penetrant inhibitor LRRK2, with IC50 of 2.6 nM in human PBMCs. LRRK2-IN-3 can be used for the research of Parkinson's disease.
    LRRK2-IN-3
  • HY-156167
    LRRK2-IN-10
    		Inhibitor
    LRRK2-IN-10 (compound 34) is a potent, mutation-selective, and brain penetrant G2019S-LRRK2 kinase inhibitor with IC50s of 11 nM and 5.2 nM for G2019S-LRRK2 pS935 and G2019S-LRRK2 pS1292, respectively. LRRK2-IN-10 has the potential for Parkinson's disease research.
    LRRK2-IN-10
  • HY-B0792A
    CZC-54252 hydrochloride
    		Inhibitor 98.44%
    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.
    CZC-54252 hydrochloride
  • HY-158365
    LRRK2-IN-14
    		Inhibitor
    LRRK2-IN-14 (Compound 8) is an orally active LRRK2 inhibitor. LRRK2-IN-14 has an IC50 of 6.3 nM for LRRK2(G2019S) cell activity.LRRK2-IN-14 has an inhibitory effect on hERG (IC50=22 μM). LRRK2-IN-14 has blood-brain barrier permeability.
    LRRK2-IN-14
  • HY-153103
    LRRK2/NUAK1/TYK2-IN-1
    		Inhibitor
    LRRK2/NUAK1/TYK2-IN-1 (conpound 226) shows inhibitory activity toward LRRK2 (Wt), LRRK2 (G2019), TYK2 and NUAK1, with IC50 values lower than 10 nM. LRRK2/NUAK1/TYK2-IN-1 can be used for autoimmune disease research.
    LRRK2/NUAK1/TYK2-IN-1
  • HY-151444
    LRRK2-IN-6
    		Inhibitor
    LRRK2-IN-6 (compound 22) is a potent, orally active, selective leucine rich repeat protein kinase 2 gene (LRRK2) inhibitor with IC50 values of 4.6 and 49 μM for GS LRRK2 and WT LRRK2, respectively. LRRK2-IN-6 inhibits LRRK2 Ser1292 and Ser925 autophosphorylation. LRRK2-IN-6 can cross the blood-brain barrier.
    LRRK2-IN-6
  • HY-144074
    LRRK2-IN-4
    		Inhibitor
    LRRK2-IN-4 is a potent, selective, CNS-penetran and orally active leucine-rich repeat kinase 2 (LRRK2) inhobitor with an IC50 of 2.6 nM. LRRK2-IN-4 has the potential for the research of Parkinson’s disease.
    LRRK2-IN-4
  • HY-148353
    PF-06455943
    		Inhibitor
    PF-06455943 is a leucine rich repeat kinase 2 (LRRK2) inhibitor with IC50 value of 3 nM. PF-06455943 also is a PET radioligand. PF-06455943 can be used for the research of ADME/neuro PK characterization and Parkinson disease (PD).
    PF-06455943
  • HY-151441
    LRRK2-IN-5
    		Inhibitor
    LRRK2-IN-5 (compound 25) is a potent, orally active, selective leucine rich repeat protein kinase 2 gene (LRRK2) inhibitor with IC50 values of 1.2 and 16 μM for GS LRRK2 and WT LRRK2, respectively. LRRK2-IN-5 inhibits LRRK2 Ser1292 and Ser925 autophosphorylation. LRRK2-IN-5 can cross the blood-brain barrier.
    LRRK2-IN-5
  • HY-152107A
    (R,R)-LRRK2-IN-7
    		Inhibitor
    (R,R)-LRRK2-IN-7 is the isomer of LRRK2-IN-7 (HY-152107). LRRK2-IN-7 is a potent, selective, and CNS-penetrant LRRK2 kinase inhibitor with an IC50 of 0.9 nM. LRRK2-IN-7 shows >1000-fold selectivity over other kinases, ion channels, and CYP enzymes.
    (R,R)-LRRK2-IN-7
  • HY-134562
    PF-06371900
    		Inhibitor
    PF-06371900 is a potent and highly selective leucine rich repeat kinase 2 (LRRK2) inhibitor.
    PF-06371900
Cat. No. Product Name / Synonyms Application Reactivity