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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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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V111107 | Lu AF58786 | 1632368-13-8 | Lu AF58786 is a highly effective and selective LRRK2 inhibitor with an IC50 value of 12 nM. |
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V88566 | LY2023-001 | 327031-30-1 | LY2023-001 is a potent G2019S LRRK2 inhibitor with IC50 of 12.9 nM. |
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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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V98092 | Nictide | 1159973-22-4 | Nictide is a peptide substrate of LRRK2 (leucine-rich repeat protein kinase 2). |
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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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V143358 | PROTAC LRRK2 Degrader-1 | 3031514-69-6 | PROTAC LRRK2 Degrader-1 is a PROTAC degrader rich in leucine repeat kinase 2 (LRRK2) with an IC50 value of less than 10 nM. |
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V143359 | PROTAC LRRK2 Degrader-2 | 3080678-93-6 | PROTAC LRRK2 Degrader-2 is a PROTAC-based LRRK2 degrader with a half-maximum concentration (DC50) of 0.14 nM. |
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V117046 | PROTAC LRRK2 Degrader-3 | 3080678-98-1 | PROTAC LRRK2 Degrader-3 is a PROTAC LRRK2 degrader with a DC50 of 0.17 nM. |
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V116492 | PROTAC LRRK2 Degrader-4 | 2839664-99-0 | PROTAC LRRK2 Degrader-4 is a PROTAC LRRK2 degrader with a DC50 of 0.79 nM. |
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V143360 | PROTAC LRRK2 Degrader-5 | 2839665-11-9 | PROTAC LRRK2 Degrader-5 is an LRRK2 PROTAC degrader. |
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V144232 | RN277 | RN277 is an LRRK2 type II kinase inhibitor. | |
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V144233 | RN341 | RN341 is a specific type II kinase inhibitor that inhibits the activity of LRRK2 (IC50: 296 nM). | |
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V145256 | SRI-31255 | 905580-86-1 | SRI-31255 is an orally effective LRRK2 inhibitor with IC50 values of 520 nM for wild-type (WT) and 427 nM for mutant G2019S. |
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