g2019s lrrk2

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.

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

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.

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.

PF-06454589 is a potent inhibitor of LRRK2.

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.

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

CZC-54252 is a potent inhibitor of LRRK2.

LRRK2-IN-17 is an orally active LRRK2 inhibitor with IC50 values of 3.5 nM for WT and 3.3 nM for G2019S, and it also inhibits RET kinase with an IC50 of 59 nM. LRRK2-IN-17 is utilized in research related to cancer and Parkinson's disease (PD).

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.

RN341 is a LRRK2-specific type II kinase inhibitor (IC50 of 296 nM). It prevents the phosphorylation of LRRK2 by stabilizing an open conformation, thereby avoiding S935 dephosphorylation. Additionally, RN341 rescues LRRK2-mediated kinesin motility blockage by preventing microtubule binding. This compound effectively inhibits both wild-type and G2019S LRRK2 at the cellular level, offering a novel avenue for Parkinson's disease research.

GSK2578215A is a potent and selective LRRK2 kinase inhibitor.

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.

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

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.

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

PF-06456384 trihydrochloride is a highly efficient and selective NaV1.7 inhibitor (IC50 = 0.01 nM), acting through protein-ligand binding rather than inhibiting the associated sodium channel. It is specifically designed for intravenous infusion and can be used in pain research.

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].

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].

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].

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.