Lys05 化学特性,用途語,生産方法
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 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.
Lys05 上流と下流の製品情報
原材料
準備製品