lrrk 2

BIX 02565 is a potent inhibitor of ribosomal S6 kinase 2 (RSK2, IC50: 1.1 nM).

CCG-1423, a selective RhoA pathway inhibitor, suppresses SRF-mediated transcription.

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).

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

LRRK2-IN-16 (compound 25) is an inhibitor of the LRRK2 kinase with an IC50 value of less than 5 μM. It is applicable for research in neurodegenerative and autoimmune diseases.

SRI-31255 is an orally active LRRK2 inhibitor, with IC50 values of 520 nM for human wild-type (WT) and 427 nM for the G2019S mutant. It inhibits kinase activity by binding to the ATP-binding pocket of LRRK2, providing neuroprotective effects. SRI-31255 serves as a lead compound for developing LRRK2-targeted therapies for Parkinson’s disease research.

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).

URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19/42/14/150 nM, for MLK1/MLK2/MLK3/DLK), and also inhibits LRRK2 activity (IC50: 11 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.

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.

LRRK2-IN-10 (compound 34) is a potent, mutation-selective, brain-penetrant inhibitor targeting G2019S-LRRK2 kinase with IC50 values of 11 nM for G2019S-LRRK2 pS935 and 5.2 nM for G2019S-LRRK2 pS1292, holding promise for research into Parkinson's disease [1].

MK-1468, a highly selective and brain-penetrant LRRK2 inhibitor, exhibits an IC50 of 0.8 nM and is utilized in the study of Parkinson's disease [1].

LRRK2 inhibitor 1 is a selective and potent LRRK2 inhibitor with an IC50 of 13 nM.LRRK2 inhibitor 1 inhibits DCLK1 kinase with an IC50 value of 2.61 nM.

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