LRRK2

Leucine-rich repeat kinase 2

LRRK2

Related Products

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.

LRRK2 Inhibitors (37)

LRRK2 Related Products (37):

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-142647

EB-42486	Inhibitor	99.62%
EB-42486 is a novel, potent, and highly selective G2019S-LRRK2 inhibitor (IC₅₀ < 0.2 nM).

HY-111493

LRRK2 inhibitor 1	Inhibitor	99.93%
LRRK2 inhibitor 1 is a potent, selective and oral LRRK2 inhibitor with an pIC₅₀ of 6.8.

HY-152107

LRRK2-IN-7	Inhibitor	98.04%
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.

HY-145317

LRRK2-IN-2	Inhibitor
LRRK2-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.

HY-153058

LRRK2-IN-8	Inhibitor
LRRK2-IN-8 is a LRRK2 inhibitor. LRRK2-IN-8 inhibits LRRK2 (wt) and LRRK2 (G2019) with IC₅₀s lower than 10 nM, and inhibits TYK2 and NUAK1 with IC₅₀s of 10-100 nM.

HY-145318

LRRK2-IN-3	Inhibitor
LRRK2-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.

HY-156167

LRRK2-IN-10	Inhibitor
LRRK2-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.

HY-B0792A

CZC-54252 hydrochloride	Inhibitor	98.44%
CZC-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.

HY-153103

LRRK2/NUAK1/TYK2-IN-1	Inhibitor
LRRK2/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.

HY-151444

LRRK2-IN-6	Inhibitor
LRRK2-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.

HY-144074

LRRK2-IN-4	Inhibitor
LRRK2-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.

HY-148353

PF-06455943	Inhibitor
PF-06455943 is a leucine rich repeat kinase 2 (LRRK2) inhibitor with IC₅₀ value of 3 nM. PF-06455943 also is a PET radioligand. PF-06455943 can be used for the research of ADME/neuro PK characterization and Parkinson disease (PD).

HY-151441

LRRK2-IN-5	Inhibitor
LRRK2-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.

HY-152107A

(R,R)-LRRK2-IN-7	Inhibitor
(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.

HY-134562

PF-06371900	Inhibitor
PF-06371900 is a potent and highly selective leucine rich repeat kinase 2 (LRRK2) inhibitor.

HY-155150

JH-XII-03-02	Inhibitor
JH-XII-03-02 is a potent and selective LRRK2 PROTAC degrader. JH-XII-03-02 can be used for parkinson's Disease (PD)?research.

HY-15800

CZC-25146 hydrochloride	Inhibitor
CZC-25146 hydrochloride is a potent LRRK2 inhibitor with IC₅₀ values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 hydrochloride inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. CZC-25146 hydrochloride prevents mutant LRRK2-induced injury of neurons in vitro. CZC-25146 hydrochloride exhibits relatively favorable pharmacokinetic properties in mice. CZC-25146 hydrochloride can increase normal α-1-antitrypsin (AAT) secretion and reduce inflammatory cytokines. CZC-25146 hydrochloride can be used to research Parkinson's disease and liver diseases.

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