SML2097

Lys05

≥98% (HPLC)

• Synonyme(s) : 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
• Formule empirique (notation de Hill): C₂₃H₂₃Cl₂N₅ · 3HCl
• Numéro CAS: 1391426-24-6
• Poids moléculaire : 549.75
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Pureté: ≥98% (HPLC)
• Forme: powder
• Conditions de stockage: desiccated
• Couleur: white to beige
• Solubilité: DMSO: 2 mg/mL, clear
• Température de stockage: −20°C

Description

Application

Lys05 has been used as an autophagy inhibitor to study its interactions with piperazine. It has also been used as a lysosomal inhibitor to study its effects on myogenesis in Gallus gallus.

Actions biochimiques/physiologiques

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 μM treatment in LN229 glioblastoma cells vs. <6.4 with 100 μM CQ or HCQ). Lys05 also shows higher anticancer activity both in vitro (IC50 3.6-6.0 μM vs. 15.6-23.8 μM 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.

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable