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Lys05

CAS No. : 1391426-24-6

MCE 站：Lys05

产品活性：Lys05 (Lys01 trihydrochloride) 是新颖的溶酶体自噬 (lysosomal autophagy) 抑制剂。在MTT试验中，对1205Lu, c8161, LN229 和HT-29细胞系的IC₅₀值分别为3.6, 3.8, 6 和7.9 μM。

研究领域：Autophagy

作用靶点：Autophagy

In Vitro: Lys01, is a 10-fold more potent autophagy inhibitor than HCQ. Compared with HCQ, Lys05, a water-soluble salt of Lys01, more potently accumulates within and deacidifies the lysosome. Lys01 and Lys05 produce equivalent dose-dependent increases in the LC3II/LC3I ratio, accumulation of the autophagy cargo protein p62, and identical IC₅₀ values in the MTT assay.

In Vivo: With this high-dose, short-term treatment, no mice die, but after 2 d of dosing, mice treated with Lys05 76 mg/kg i.p. are observed to have arched backs and lethargy. Morphologically, EM show that cells with intact nuclear and cytoplasmic membranes contain large AVs in Lys05-treated tumors. Tumor growth is significantly impaired in Lys05-treated tumors compared with controls. Lys05 treatment results in a 53% reduction in the average daily tumor growth rate compared with vehicle-treated controls. A significant three- and six-fold accumulation of AV is observed at the end of 14 d of treatment in HCQ- and Lys05-treated tumors, respectively, compared with control-treated tumors.

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