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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CZC-54252 hydrochloride
0 ImagesCZC-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.
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Lu AF58786
0 ImagesCat. No.: HY-180320CAS No.: 1632368-13-8Lu AF58786 is a potent and selective LRRK2 inhibitor with an IC50 of 12 nM. Lu AF58786 also exhibits inhibition activity against LRRK2 G2019S and LRRK2 A2016T with IC50s of 19 and 93 nM. Lu AF58786 inhibits phosphorylation of LRRK2, Rab10 and Rab12 in human peripheral blood mononuclear cells. Lu AF58786 can be used for parkinson’s disease research.
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LRRK2-IN-14
0 ImagesCat. No.: HY-158365CAS No.: 2942328-06-3
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PROTAC LRRK2 Degrader-1
0 ImagesCat. No.: HY-171801CAS No.: 3031514-69-6PROTAC LRRK2 Degrader-1 (compound 18) is a leucine-rich repeat kinase 2 (LRRK2) PROTAC degrader with an IC50 value less than 10 nM. PROTAC LRRK2 Degrader-1 can be used in the research of Parkinson's disease.
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LRRK2/NUAK1/TYK2-IN-1
0 ImagesCat. No.: HY-153103CAS No.: 2629192-96-5LRRK2/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.
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LRRK2-IN-6
0 ImagesCat. No.: HY-151444CAS No.: 2892451-17-9LRRK2-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.
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SRI-29132
0 ImagesCat. No.: HY-165543CAS No.: 1482305-44-1SRI-29132 is a potent leucine-rich repeat kinase 2 (LRRK2) inhibitor. SRI-29132 is promising for research of Parkinson’s disease.
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LRRK2-IN-20
0 ImagesCat. No.: HY-175651CAS No.: 2763594-19-8LRRK2-IN-20 (EX. 4.64) is a LRRK2 inhibitor with a pIC50 of 0.7921 nM. LRRK2-IN-20 can be used in Parkinson's disease (PD) research.
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LRRK2-IN-4
0 ImagesCat. No.: HY-144074CAS No.: 2641054-59-1LRRK2-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.
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LRRK2-IN-19
0 ImagesCat. No.: HY-177016CAS No.: 2839667-09-1LRRK2-IN-19 is a PROTAC target protein ligand that can be used to synthesize PROTAC JH-XII-03-02 (HY-155150). JH-XII-03-02 is a highly potent and selective LRRK2 PROTAC degrader, which can be used in Parkinson's disease research.
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LRRK2-IN-5
0 ImagesCat. No.: HY-151441CAS No.: 2892451-45-3LRRK2-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.
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LRRK2/JNK3-IN-1
0 ImagesCat. No.: HY-184652LRRK2/JNK3-IN-1 is a brain-penetrant multi-target inhibitor of LRRK2 (including G2019S mutant and wild-type) and JNK3, with enzymatic IC50 values of 3.90 nM against LRRK2G2019S, 3.24 nM against wild-type LRRK2, and 22.1 nM against JNK3. LRRK2/JNK3-IN-1 displays favorable selectivity in a 97-kinase profiling screen, and also shows inhibitory activity against JNK1, JNK2, and MKNK2. LRRK2/JNK3-IN-1 can be used for the research of Parkinson's disease.
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STF-3600
0 ImagesCat. No.: HY-189065CAS No.: 2765654-79-1STF-3600 is a LRRK2G2019S inhibitor with an IC50 of 0.9 nM against the human target. It has oral activity and can cross the blood-brain barrier. STF-3600 selectively inhibits kinase activity, including autophosphorylation at Ser935 and Ser1292, as well as phosphorylation of the endogenous substrate Rab10 at Thr73. STF-3600 inhibits vacuolization of type II pulmonary epithelial cells in wild-type/heterozygous mice, while it induces this vacuolization phenotype in homozygous mice. STF-3600 can be used in Parkinson's disease research.
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LRRK2-IN-15
0 ImagesCat. No.: HY-168041LRRK2-IN-15 is an LRRK2 inhibitor. The IC50 value for PBMC cells is 5 nM, and the IC50 value for BCRP is 1.5 μM. LRRK2-IN-15 can be used for research on Parkinson's disease.
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LY2023-001
0 ImagesCat. No.: HY-162699CAS No.: 327031-30-1
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LRRK2-IN-13
0 ImagesCat. No.: HY-161571CAS No.: 3032733-17-5LRRK2-IN-13 (Compound 13) is an inhibitor of LRRK2 (IC50=0.57 nM). LRRK2-IN-13 has brain penetrating properties.
