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You are here:Home-Inhibitors & Agonists-Autophagy-LRRK2

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    Leucine-rich repeat kinase 2 (LRRK2) is an enzyme that in humans is encoded by the PARK8 gene. LRRK2 is a member of the leucine-rich repeat kinase family. Variants of this gene are associated with an increased risk of Parkinson's disease (PD)and also Crohn's disease (CD).


    Leucine-rich repeat kinase 2 (LRRK2) is the gene responsible for autosomal-dominant PD, PARK8, which is originally defined by linkage analysis of a Japanese family. LRRK2 is a complex kinase consisting of LRR, ROC, COR, kinase, and WD40 domains. LRRK2 plays a key role in axonal extension, autophagy, proliferation, and survival of neurons. In addition to neurons, LRRK2 is highly expressed in immune cells such as B cells, macrophages, and microglia. Several studies have demonstrated that LRRK2 is related to inflammatory responses of microglia that could be involved in the development and progression of neurodegeneration.


      LRRK2 is a large, multidomain protein containing two catalytic domains: a Ras of complex proteins (Roc) G-domain and a kinase domain. Leucine-rich repeat kinase 2 (LRRK2) represents a promising drug target for treatment and prevention of Parkinson’s disease (PD), because mutations in LRRK2 are the most common cause of Mendelian forms of the disease. PD-associated LRRK2 variants show decreased GTPase and increased kinase activity.

Cat. No. Product Name CAS No. Information
GY04445

JH-II-127

 		1700693-08-8

A potent and selective inhibitor of both wild-type and G2019S mutant LRRK2 with IC50 of 6.6 and 2.2 nM, respectively; also inhibits LRRK2 A2016T with IC50 of 47.7 nM; substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at 0.1-0.3 uM in a variety of cell types; inhibits Ser935 phosphorylation in mouse brain; orally active.
GY04384

GSK2578215A

 		1285515-21-0

GSK2578215A is a highly potent, selective, BBB-permeable LRRK2 inhibitor with IC50 of 10.9 and 9.9 nM for wild-type LRRK2 and the G2019S mutant, respectively; shows 8-fold reduced potentcy against A2016T mutant LRRK2 (IC50=81 nM); inhibits Ser910 and Ser935 phosphorylation in both wild-type LRRK2 and LRRK2 G2019S stably transfected into HEK293 cells at 0.1-0.3 uM, also induces dephosphorylation of Ser910 and 935 at 1-3 μM in the inhibitor-resistant LRRK2[A2016T+ G2019S] and LRRK2 [A2016T] mutants; induces protective autophagy in SH-SY5Y cells.
GY04383

GNE0877

 		1374828-69-9

GNE-0877 is a highly potent, selective, brain penetrant LRRK2 inhibitor with Ki of 0.7 nM, pLRRK2 IC50 of 3 nM; dispalys excellent selectivity against 178-membered Invitrogen kinase panel, as well as a representative panel of receptors and ion channels; demonstrates robust concentration-dependent inhibition of LRRK2 Ser1292 autophosphorylation (IC50=3 nM) in BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation.
GY04038

GNE9605

 		1536200-31-3

GNE-9605 is a highly potent, selective, brain penetrant LRRK2 inhibitor with Ki of 2 nM, pLRRK2 IC50 of 19 nM; dispalys excellent selectivity against 178-membered Invitrogen kinase panel, as well as a representative panel of receptors and ion channels; demonstrates robust concentration-dependent inhibition of LRRK2 Ser1292 autophosphorylation (IC50=20 nM) in BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation.
GY04018

PF-06447475

 		1527473-33-1

PF-06447475 is a highly potent, selective, brain penetrant LRRK2 kinase inhibitor with IC50 of 3 and 11nM for WT LRRK2 and G2019S mutant, respectively; PF-06447475 is also sufficiently potent in the LRRK2 whole cell assay with IC50 of 25 nM; protects nerve-like differentiated cells (NLCs) against rotenone induced noxious effect, prevents α-synuclein-induced neurodegeneration in rats.
GY05205

GNE-7915 tosylate

 		2070015-00-6

GNE-7915 tosylate (GNE7915 tosylate) is a highly potent, selective, and brain-penetrable LRRK2 inhibitor with IC50 of 1.9 nM; shows 1/187 kinases with 50% inhibition at 0.1 uM; possesses an ideal balance of LRRK2 cellular potency, broad kinase selectivity, metabolic stability, and brain penetration across multiple species.

GY04244

GNE-7915

 		1351761-44-8

GNE-7915 is a highly potent, selective, and brain-penetrant LRRK2 inhibitor with IC50 of 1.9 nM; shows 1/187 kinases with 50% inhibition at 0.1 uM; possesses an ideal balance of LRRK2 cellular potency, broad kinase selectivity, metabolic stability, and brain penetration across multiple species.
GY04216

LRRK2-IN-1

 		1234480-84-2

LRRK2-IN-1 is a potent LRRK2 inhibitor with IC50s of 13 nM/6 nM for wild-type/G2019S mutant LRRK2 repectively (0.1 mM ATP in the assay); shows modest activity against LRRK2 A2016T (IC50=2.45 uM) and LRRK2 A2016T+G2019S mutant (IC50=3.08 uM); also inhibits DCLK1 (IC50=2.61 nM) and 2 (IC50=45 nM); induces dephosphorylation of Ser910 and Ser935 of LRRK2 and alters the cytoplasmic localisation of LRRK2.

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