Synonyms: Lys-01 3HCl; Lys-05; Lys01 3HCl; N-(7-Chloroquinolin-4-yl)-N'-[2-[(7-chloroquinolin-4-yl)amino]ethyl]-N'-methylethane-1,2-diamine trihydrochloride; N1-(7-Chloroquinolin-4-yl)-N2-[2-[(7-chloroquinolin-4-yl)amino]ethyl]-N2-methylethane-1,2-diamine trihydrochloride; PS-1001; PS1001
Molecular Formula: C23H23Cl2N5 · 3HCl
Molecular Weight: 549.75
Linear Structural Formula: C23H23Cl2N5 · 3HCl
Purity: >=98% (HPLC)
Storage: -20C
Biochem Physiol Actions: Lys05 (Lys01 trihydrochloride) is a dimeric chloroquine (CQ) that deacidifies the lysosome and causes impairment of lysosomal enzymes, exhibiting more than 10-fold higher autophagy inhibitory potency than hydroxychloroquine (HCQ) and CQ (LC3II/LC3I ratio = 15.4 post 4 hr 10 muM treatment in LN229 glioblastoma cells vs. <6.4 with 100 mum cq or hcq). lys05 also shows higher anticancer activity both in vitro (ic50 3.6-6.0 mum vs. 15.6-23.8 mum with hcq in 1205lu, c8161, ln229, ht-29 cultures) and in mice in vivo (ec50 in reducing tumor growth rate>=10 mg/kg/day i.p.; HT29 xenografts) with toxicity observed only at high doses (>=80 mg/kg) as a result of significant lysozyme reduction.