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。

Lys05 (Lys01 trihydrochloride) is a novel lysosomal autophagy inhibitor with IC 50 values of 3.6, 3.8, 6 and 7.9 μM for 1205Lu, c8161, LN229 and HT-29 cell line in the MTT assay.

Solid

IC50: 3.6 μM (1205Lu), 3.8 μM (c8161), 6 μM (LN229), 7.9 μM (HT-29)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. McAfee Q, et al. Autophagy inhibitor Lys05 has single-agent antitumor activity and reproduces the phenotype of a genetic autophagy deficiency. Proc Natl Acad Sci U S A. 2012 May 22;109(21):8253-8.

In Vitro: DMSO : 25 mg/mL (45.48 mM; ultrasonic and adjust pH to 2 with HCl)H₂O : 6.4 mg/mL (11.64 mM; Need ultrasonic)配制储备液