Lys05 Chemische Eigenschaften,Einsatz,Produktion Methoden
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 Upstream-Materialien And Downstream Produkte
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Downstream Produkte