lrrk2 in 1

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

LRRK2 NUAK1 TYK2-IN-1 (compound 226) exhibits inhibitory activity against LRRK2 (Wt), LRRK2 (G2019), TYK2, and NUAK1, demonstrating IC50 values below 10 nM. This compound is useful for research into autoimmune diseases.

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].

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].

JH-XII-03-02 is a potent, selective leucine-rich repeat kinase 2 (LRRK2) proteolysis targeting chimera (PROTAC) degrader, utilized in Parkinson's Disease (PD) research [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].

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].