LRRK2-IN-1

LRRK2-IN-1 is a **potent and selective small molecule inhibitor of leucine-rich repeat kinase 2 (LRRK2)**, designed primarily for research applications in Parkinson's disease and related disorders. It acts as an ATP-competitive kinase inhibitor, selectively targeting both wild-type and mutant (notably G2019S) LRRK2 enzymes, which are implicated in familial and sporadic forms of Parkinson’s disease[1][4]. LRRK2-IN-1 demonstrates strong inhibitory activity in vitro, with reported IC50 values in the low nanomolar range (WT: 13 nM; G2019S: 6 nM)[1]. Mechanistically, the compound binds in the ATP pocket of LRRK2 and competes at the active (type I) kinase conformation site, leading to reduced phosphorylation of LRRK2 substrates[1][4]. Though primarily used as a chemical probe in laboratory studies—including radiolabeling for autoradiography and binding assays—it plays a significant role in elucidating LRRK2 biology and as proof-of-concept for therapeutic inhibition of LRRK2 in Parkinson's disease models[1]. There is no evidence that LRRK2-IN-1 has undergone clinical development or commercial distribution as a therapeutic; its principal use is preclinical and scientific research[1][4].