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LRRK2

LRRK2

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.

LRRK2 related products

Structure Cat No. Product Name CAS No. Product Description
CZC-25146 V3738 CZC-25146 1191911-26-8 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.
CZC-25146 freebase V2153 CZC-25146 freebase 1191911-26-8 CZC-25146 is a potent and selective LRRK2 inhibitor.
CZC-25146盐酸盐 V3739 CZC-25146 HCl 1191911-26-8 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.
CZC-54252 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.
CZC54252 HCl 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).
GNE-7915 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.
GNE-7915甲苯磺酸盐 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.
GNE-9605 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.
GNE0877 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.
GSK-2578215 A 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.
HG-10-102-01 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.
LRRK2-IN-12 V88565 LRRK2-IN-12 3032733-05-1 LRRK2-IN-12 (compound 1) inhibits the activity of LRRK2 G20195 (IC50=0.45 nM), LRRK2 WT (IC50=1.1 nM) and LRRK2 WT ADP-Glo (IC50=0.46 nM).
LRRK2-IN-13 V88563 LRRK2-IN-13 3032733-17-5 LRRK2-IN-13 (Compound 13) is an inhibitor of LRRK2 (IC50=0.57 nM).
LRRK2-IN-14 V88564 LRRK2-IN-14 2942328-06-3 LRRK2-IN-14 (Compound 8) is an orally available LRRK2 inhibitor.
LRRK2-IN-5 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.
LRRK2-IN-6 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.
LRRK2抑制剂1 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.
LY2023-001 V88566 LY2023-001 327031-30-1 LY2023-001 is a potent G2019S LRRK2 inhibitor with IC50 of 12.9 nM.
MK-1468 V75971 MK-1468 2769107-89-1 MK-1468 is a selective, brain-penetrating LRRK2 inhibitor (antagonist) with IC50 of 0.8 nM.
MLi-2 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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