leucine-rich repeat kinase 2

CZC-25146 (CHEMBL2397014) is an effective, specific and metabolically stable LRRK2 inhibitor with IC50 of 4.76/6.87 nM for wild-type LRRK2(Leucine-rich repeat kinase-2) and G2019S LRRK2, respectively.

JH-II-127 is an oral inhibitor of leucine-rich repeat kinase 2 (LRRK2), targeting WT LRRK2, G2019S LRRK2, and A2016T LRRK2 with IC50 values of 6.6 nM, 2.2 nM, and 47.7 nM, respectively.

MLi-2 is a structurally novel, highly potent, and selective LRRK2 kinase inhibitor with central nervous system activity. MLi-2 exhibits exceptional potency in a purified LRRK2 kinase assay in vitro (IC50 = 0.76 nM), a cellular assay monitoring dephosphorylation of LRRK2 pSer935 LRRK2 (IC50 = 1.4 nM), and a radioligand competition binding assay (IC50 = 3.4 nM).

PFE-360 (PF-06685360) is a potent and selective inhibitor of LRRK2 kinase, with an in vivo IC50 of 2.3 nM.

GNE-9605 is a highly effective, specifical, and brain-penetrant LRRK2 inhibitor (IC50: 19 nM).

GNE-7915 is a highly potent, selective and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) inhibitor.

CZC-54252 is a potent inhibitor of LRRK2.

PF-06447475 is a highly effective, specific, brain penetrant LRRK2 inhibitor with IC0 of 3/11 nM for wild type LRRK2 and G2019S LRRK2 respectively.

GSK2578215A is a potent and selective LRRK2 kinase inhibitor.

LRRK2-IN-1 is an effective and selective LRRK2 inhibitor.

CZC-54252 hydrochloride is a selective inhibitor of LRRK2 with IC50s of 1.85 nM and 1.28 nM for wild-type and G2019S LRRK2. CZC-54252 hydrochloride has a neuroprotective activity and attenuates G2019S LRRK2-induced human neuronal injury with an EC50 of 1 nM.

EB-42486 is an effective and highly selective inhibitor of G2019S-LRRK2 with an IC50 < 0.2 nM.

CZC-25146 is a selective LRRK2 inhibitor with IC50 of 4.76 nM/6.87 nM for wild type LRRK2 and G2019S LRRK2, respectively.

GNE0877 (GNE 0877) is a highly effective and specific leucine-rich repeat kinase 2 (LRRK2) inhibitor (Ki: 0.7 nM).

IKK 16 (IKK Inhibitor VII) is a selective IκB kinase (IKK) inhibitor for IKK-2, IKK complex and IKK-1 with IC50 of 40 nM, 70 nM and 200 nM, respectively.

HG-10-102-01 is an inhibitor of leucine-rich repeat kinase 2 (LRRK2, IC50 of 20.3 nM).

PF-06454589 is a potent inhibitor of LRRK2.

IKK 16 hydrochloride is a selective inhibitor of IKK2 (IC50: 40 nM), the IKK complex (IC50: 70 nM), and IKK1 IκB kinase (IKK) (IC50: 200 nM), as well as leucine-rich repeat kinase-2 (LRRK2; IC50: 50 nM).

LRRK2-IN-6 (compound 22) is an orally active, selective leucine-rich repeat protein kinase 2 (LRRK2) inhibitor with blood-brain barrier permeability, inhibiting GS LRRK2 (IC50: 4.6 μM) and WT LRRK2 (IC50: 49 μM). LRRK2-IN-6 exhibited inhibitory effects on the autophosphorylation of LRRK2 at Ser1292 and Ser925.

LRRK2-IN-5 (compound 25) is an orally active, blood-brain barrier-penetrating, selective leucine-rich repeat protein kinase 2 (LRRK2) inhibitor, effective for GS LRRK2 (IC50: 1.2 μM) and WT LRRK2 (IC50: 16 μM), and can inhibit the autophosphorylation of LRRK2 at Ser1292 and Ser925.

LRRK2-IN-4 is a potent, selective, orally active leucine-rich repeat kinase 2 (LRRK2) inhibitor that crosses the blood-brain barrier with an IC50 value of 2.6 nM. LRRK2-IN-3 has shown investigational potential in [Parkinson's disease].

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

PF-06455943, a leucine rich repeat kinase 2 (LRRK2) inhibitor, exhibits an inhibition concentration (IC50) value of 3 nM and also functions as a PET radioligand. It is utilized in the research of ADME/neuro PK characterization and Parkinson's disease (PD).

XL01126 is a potent degrader of leucine-rich repeat kinase 2 (LRRK2), exhibiting DC50 values of 14 nM for G2019S LRRK2 and 32 nM for wild-type LRRK2. XL01126 is capable of crossing the blood-brain barrier and serves as a degrader probe for Parkinson’s disease research. XL01126 is also a valuable molecular tool for investigating the non-catalytic and scaffolding functions of LRRK2. These properties support the utilization of XL01126 in studies of protein degradation technologies, neurodegenerative disease biology, and LRRK2-mediated cellular signaling pathways.