lrrk2 inhibitor 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.

CZC-54252 is a potent inhibitor of LRRK2.

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.

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

GSK2646264 (Compound 44) is a highly effective and specific inhibitor of spleen tyrosine kinase (SYK) with a pIC50 of 7.1. It also inhibits multiple kinases, including LCK (pIC50 5.4), LRRK2 (pIC50 5.4), GSK3β (pIC50 5.3), JAK2 (pIC50 5), VEGFR2 (pIC50 4.5), Aurora B (pIC50 <4.6), and Aurora A (pIC50 <4.3). Notably, GSK2646264 demonstrates skin penetrability, reaching both the epidermis and dermis [1].

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.

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-IN-12 (compound 1) is a potent inhibitor of LRRK2 (G20195) with an IC 50 of 0.45 nM, LRRK2 WT with an IC 50 of 1.1 nM, and LRRK2 WT ADP-Glo with an IC 50 of 0.46 nM. This compound is utilized in research related to Alzheimer's Disease [1].

LRRK2-IN-13 (Compound 13), with an IC50 value of 0.57 nM, serves as an inhibitor of LRRK2 and exhibits properties that allow it to penetrate the brain [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].