产品描述: | Lys05 (Lys01 trihydrochloride) is a novel lysosomal autophagy inhibitor with IC50 values of 3.6, 3.8, 6 and 7.9 μM for 1205Lu, c8161, LN229 and HT-29 cell line in the MTT assay. |
靶点: |
IC50: 3.6 μM (1205Lu), 3.8 μM (c8161), 6 μM (LN229), 7.9 μM (HT-29);lysosomalautophagy; Autophagy |
体外研究: |
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 |
体内研究: |
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 |
参考文献: |
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. |
溶解性: |
Soluble in DMSO、H2O |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
1.819 ml |
9.095 ml |
18.19 ml |
5 mM |
0.364 ml |
1.819 ml |
3.638 ml |
10 mM |
0.182 ml |
0.91 ml |
1.819 ml |
50 mM |
0.036 ml |
0.182 ml |
0.364 ml |
|
注意: |
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