lrrk2 (g2019s)

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

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

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

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.

PF-06454589 is a potent inhibitor of LRRK2.

ERK5-IN-1 is a potent ERK5 inhibitor (IC50: 87 nM) and also inhibits LRRK2[G2019S] (IC50: 26 nM).

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.

CZC-54252 is a potent inhibitor of LRRK2.

XL01126, a potent degrader of LRRK2, exhibits DC50 values of 14 nM (G2019S LRRK2) and 32 nM (WT LRRK2), respectively. It has the ability to cross the blood-brain barrier, making it a viable degrader probe for Parkinson's disease research. This compound is instrumental in exploring the non-catalytic and scaffolding functions of LRRK2 [1].

Nictide, a peptide substrate for LRRK2 (leucine-rich repeat protein kinase-2), undergoes phosphorylation by the activated form of LRRK2[G2019S], exhibiting a Km value of 10 μM.

LRRK2-IN-14 (Compound 8), an orally active inhibitor of LRRK2, exhibits an IC 50 of 6.3 nM against LRRK2(G2019S) cell activity and demonstrates inhibitory effects on hERG with an IC 50 of 22 μM. Additionally, LRRK2-IN-14 is permeable to the blood-brain barrier [1].

GSK2578215A is a potent and selective LRRK2 kinase inhibitor.

Lu AF58786 is a novel potent and selective inhibitor of LRRK2, inhibiting LRRK2 WT, the overactive variant G2019S, and the resistant mutant A2016T56 at 12 nM, 19 nM and 93 nM, respectively.

PF-06447475 trihydrochloride is a potent, selective LRRK2 kinase inhibitor that demonstrates excellent brain penetration, exhibiting IC50 values of 3 nM for wild-type LRRK2 and 11 nM for G2019S LRRK2 variants. It holds potential for Parkinson's disease (PD) research [1].

XMD17-109 (ERK5-IN-1) is a new selective ERK-5 inhibitor (EC50: 4.2 uM, HEK293 cells).

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.

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

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

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].