LRRK2
Leucine-rich repeat kinase 2
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.
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LRRK2 Related Products (74)
Related Products (74)
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Antibodies (1)
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LRRK2-IN-7
0 ImagesLRRK2-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.
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MK-1468
0 ImagesMK-1468 is an orally active, selective, and BBB-permeable LRRK2 inhibitor. MK-1468 can be used for the research of Parkinson's disease.
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EB-42486
0 ImagesEB-42486 is a novel, potent, and highly selective G2019S-LRRK2 inhibitor (IC50: < 0.2 nM). EB-42486 can be used in the research of Parkinson's disease.
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JH-II-127
0 ImagesJH-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.
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GSK2646264
0 ImagesGSK2646264 (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, Aurora B and Aurora A, respectively. GSK2646264 is penetrable into the epidermis and dermis of the skin.
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PF-06454589
0 ImagesPF-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.
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SRI-31255
0 ImagesSRI-31255 is an orally active LRRK2 inhibitor with IC50 values of 520 and 427 nM for human wild-type (WT) and mutant G2019S, respectively. SRI-31255 exerts neuroprotective effects by binding to the ATP-binding pocket of LRRK2, inhibiting kinase activity. SRI-31255 can be used as a lead compound for the development of LRRK2-targeted drugs for the treatment of Parkinson's disease.
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IN04
0 ImagesIN04 is a inhibitor of leucine-rich repeat kinase 1 (LRRK1). IN04 can completely block the binding of ATP to the human LRRK1 kinase domain, thereby inhibiting the kinase activity of LRRK1. IN04 can significantly impair the bone resorption ability of osteoclasts, with an IC50 value of 5.72 μM. IN04 can be used for the study of osteoporosis.
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RN341
0 ImagesRN341 is a specific type II kinase inhibitor of LRRK2 (IC50: 296 nM). RN341 inhibits LRRK2 phosphorylation and avoids S935 dephosphorylation by stabilizing the open conformation. RN341 rescues LRRK2-mediated kinesin motility block by preventing microtubule binding. RN341 effectively inhibits LRRK2 wild-type and G2019S mutant at the cellular level. RN341 provides a new direction for Parkinson's disease research.
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(R,R)-LRRK2-IN-7
0 ImagesCat. No.: HY-152107ACAS No.: 2307277-92-3(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.
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LRRK2-IN-2
0 ImagesCat. No.: HY-145317CAS No.: 2641059-19-8LRRK2-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.
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LRRK2-IN-3
0 ImagesCat. No.: HY-145318CAS No.: 2641054-60-4LRRK2-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.
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LRRK2-IN-17
0 ImagesCat. No.: HY-172952CAS No.: 2101821-86-5LRRK2-IN-17 (Compound 6) is an orally active LRRK2 inhibitor (IC50: 3.5 and 3.3 nM for WT and G2019S, respectively). LRRK2-IN-17 inhibits RET kinase (IC50: 59 nM). LRRK2-IN-17 can be used in cancer and Parkinson's disease (PD) research.
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LRRK2-IN-16
0 ImagesCat. No.: HY-169576CAS No.: 852375-30-5LRRK2-IN-16 (compound 25) is a LRRK2 kinase inhibitor with an IC50 < 5 μM. LRRK2-IN-16 can be utilized in neurodegenerative disorders and autoimmune disorders research.
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LRRK2-IN-10
0 ImagesCat. No.: HY-156167CAS No.: 2704562-80-9LRRK2-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.
