Leucine-rich repeat kinase 2 (LRRK2) is a member of the ROCO protein family that is widely expressed. LRRK2 is a multidomain, complex protein with multiple protein-protein interaction domains as well as kinase and GTPase enzymatic activities. Parkinson's disease (PD) is genetically inherited and has both familial and idiopathic forms. Vesicle trafficking, neuronal death, mitochondrial dysfunction, and inflammation are all linked to LRRK2.
Leucine-rich repeats (LRR), ankyrin repeats (ANK), Ras of complex proteins (ROC), C-terminal of Roc (COR), MAPK-like kinase, and WD40 motifs are among the multiple functional domains found in the very large protein LRRK2, which has 2527 amino acids. Both sporadic and familial PD are significantly influenced by LRRK2 mutations. The enzymatic domains of LRRK2 have a high concentration of pathogenic mutations, and kinase activity appears to be correlated with cytotoxicity, raising the possibility of kinase-based therapeutic approaches for LRRK2-associated PD. The G2019S mutation, which is the most well-known mutation to date, increases kinase activity.Mutations in the GTPase domain, like R1441C and R1441G, have also been reported to affect kinase activity.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V3738 | CZC-25146 | 1330003-04-7 | CZC-25146 is a potent, selective, and metabolically stable LRRK2 inhibitor (Leucine-rich repeat kinase-2) with IC50 of 4.76 nM and 6.87 nM for wild type LRRK2 and G2019S LRRK2 respectively. |
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V2153 | CZC-25146 freebase | 1191911-26-8 | CZC-25146 is a potent and selective LRRK2 inhibitor. |
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V3739 | CZC-25146 HCl | 1330003-04-7 | CZC-25146 is a potent, selective, and metabolically stable LRRK2 inhibitor (Leucine-rich repeat kinase-2) with IC50 of 4.76 nM and 6.87 nM for wild type LRRK2 and G2019S LRRK2 respectively. |
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V2923 | CZC-54252 | 1191911-27-9 | CZC-54252 is a potent, selective, and metabolically stable LRRK2 inhibitor (Leucine-rich repeat kinase-2) with IC50 of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2 respectively. |
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V4460 | CZC54252 HCl | 1784253-05-9 | CZC-54252 HCl (CZC54252) is a novel and potent LRRK2 (leucine-rich repeat kinase 2) inhibitor with a potential forParkinsons disease (PD). |
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V0772 | GNE-0877 | 1374828-69-9 | GNE-0877 (GNE 0877; GNE0877) is a novel, highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor with important biological activity. |
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V0773 | GNE-7915 | 1351761-44-8 | GNE-7915 (GNE 7915; GNE7915) is a novel,highly potent, selective, and brain-penetrant leucine-rich repeat kinase 2 (LRRK2) inhibitor with anti-PD (Parkinsons disease) activity. |
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V3835 | GNE-7915 tosylate | 2070015-00-6 | GNE-7915 tosylate is a novel,highly potent, selective, and brain-penetrant leucine-rich repeat kinase 2 (LRRK2) inhibitor, with IC50 and Ki of 9 nM and 1 nM, respectively. |
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V0774 | GNE-9605 | 1536200-31-3 | GNE-9605 (GNE 9605; GNE9605) is a novel, brain-penetrant,highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor with anti-PD (Parkinsons disease) activity. |
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V0775 | GSK2578215A | 1285515-21-0 | GSK2578215A (GSK-2578215A; GSK 2578215A;GSK-2578215 A) is a novel, highly potent and selective LRRK2 kinase inhibitor with anti-PD (Parkinsons disease) activity. |
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V4138 | HG-10-102-01 | 1351758-81-0 | HG-10-102-01 (LRRK2 inhibitor 1) is a novel, potent and selective inhibitor of wild-type LRRK2 (leucine-rich repeat kinase 2) with an IC50 of 23.3 nM. |
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V0776 | LRRK2-IN-1 | 1234480-84-2 | LRRK2-IN-1 (LRRK2-IN 1; LRRK2 IN-1) is a novel, highly potent and selective inhibitor of leucine-rich repeat kinase 2 (LRRK2) with anti-PD (Parkinsons disease) activity. |
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V75972 | LRRK2-IN-5 | 2892451-45-3 | LRRK2-IN-5 (compound 25) is an orally bioavailable and selective leucine-rich repeat protein kinase 2 gene (LRRK2) inhibitor (antagonist) with IC50s of 1.2 and 16 μM for GS LRRK2 and WT LRRK2, respectively. |
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V75973 | LRRK2-IN-6 | 2892451-17-9 | LRRK2-IN-6 (compound 22) is an orally bioavailable and selective leucine-rich repeat protein kinase 2 gene (LRRK2) inhibitor (antagonist) with IC50s of 4.6 and 49 μM for GS LRRK2 and WT LRRK2, respectively. |
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V75971 | MK-1468 | 2769107-89-1 | MK-1468 is a selective, brain-penetrating LRRK2 inhibitor (antagonist) with IC50 of 0.8 nM. |
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V25704 | MLi-2 | 1627091-47-7 | MLi-2 (MLi2) is a novel, highly potent, orally bioactive,and selective LRRK2 (Leucine-Rich Repeat Kinase 2) kinase inhibitor (IC50= 0.76 nM) with CNS (central nervous system) activity, and thus has the potential for treating Parkinsons disease. |
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V2916 | PF-06447475 | 1527473-33-1 | PF-06447475 (PF06447475) is a novel, highly potent, selective and brain penetrable inhibitor ofLeucine rich repeat kinase 2 (LRRK2)with anti-PD activity. |
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V3762 | PF-06454589 | 1527473-30-8 | PF-06454589 is an analog ofPF-06447475which is a highly potent, brain penetrant and selective LRRK2 inhibitor which has been profiled in in vivo safety and pharmacodynamic studies. |
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