产品说明

应用

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.

生化/生理作用

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.

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