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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
H1801	SR 9444	1442659-77-9	SR 9444 is a small molecule bidentate-binding dual inhibitor probe of the LRRK2 and JNK with IC50 of 12 nM and 99 nM respectively; shows reasonable selectivity against a panel of 116 kinases; exhibits good cell potency, inhibits LRRK2:G2019S-induced mitochondrial dysfunction in SHSY5Y cells.
H1800	PFE-360	1527475-61-1	PFE-360 is a novel potent, selective, brain-penetrating LRRK2 inhibitor with IC50 of 3 nM; induces a morphological kidney phenotype resembling that of the LRRK2 ko rats, whereas no effects in the lung; PFE-360 treatment induces morphological changes characterised by darkened kidneys and progressive accumulation of hyaline droplets in the renal proximal tubular epithelium, the estimated PFE-360 unbound plasma concentration off 10-fold the IC50 (30 nM) to achieve full peripheral LRRK2 inhibition.
H1799	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.
H1798	MLi-2	1627091-47-7	A potent, selective, orally available and brain-penetrant LRRK2 inhibitor with kinase IC50 of 0.76 nM, cellular IC50 of 1.4 nM (dephosphorylation of LRRK2 pSer935 LRRK2); displays >295-fold selectivity for over 300 kinases in addition to a diverse panel of receptors and ion channels; signficantly reduces the ratio of phosphorylated Ser935 LRRK2 (pS935) to total LRRK2 in the mouse cortex, consistent with enlarged type II pneumocytes.
H1797	LRRK2-IN-1	1234480-84-2	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.
H1796	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.
H1795	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.
H1794	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.
H1793	GNE-9605	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.
H1792	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.

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