- 产品描述： CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion
- 靶点： Apoptosis; Autophagy
- 体外研究： Treatment of human umbilical vein endothelial cells (HUVECs) with CA-5f for 1 h suppressed the levels of cytoskeletal proteins and membrane traffic proteins. CA-5f exhibited strong cytotoxicity against A549 NSCLC cells, but low cytotoxicity to normal HUVECs, by increasing mitochondrial-derived reactive oxygen species (ROS) production.
- 体内研究： CA-5f effectively suppressed the growth of A549 lung cancer xenograft as a single agent with an excellent tolerance in vivo. Results from western blot, immunofluorescence, and TdT-mediated dUTP nick end labeling (TUNEL) assays showed that CA-5f inhibited autophagic flux, induced apoptosis, and did not affect the level of CTSB (cathepsin B) and CTSD (cathepsin D) in vivo, which were consistent with the in vitro data
- 细胞实验： A549 cells or HUVECs were seeded into 100-mm culture dishes. When cells reached 80% confluency, they were exposed to DMSO or CA-5f for 6 h or 24 h. Then the cells were fixed, dehydrated, embedded, sectioned, and stained as previously described. Finally, the ultrathin sections of these samples were observed under a JEM-1230 transmission electron microscopy.
- 动物实验： Four-week-old BALB/c nude mice were purchased from Beijing Vital River Laboratory Animal Technology Co., Lt and kept in specific pathogen-free conditions at the Experimental Animal Center in the Institute of Medicine in Zhengzhou University. Nude mice underwent subcutaneous injection of A549 cells (1 × 10^6) at the right scapula. 8 days after A549 cell implantation, mice exhibited palpable tumors, then they were randomly divided into 2 groups (each group n = 5). CA-5f was injected via caudal vein every 2 days for up to 30 days. DMSO was used as a control. From the initial injection, the tumor size was measured every 2 days. Tumor volumes were calculated as tumor length × (square of width)/2. At the end of the experiment, all mice were sacrificed and the tumors were resected immediately and photographed. The weight of each tumor was measured.
- 参考文献：
1. Zhang L, et al. Identification of compound CA-5f as a novel late-stage autophagy inhibitor with potent anti-tumor effect against non-small cell lung cancer. Autophagy. 2019 Mar;15(3):391-406.
- 溶解性： Soluble in DMSO
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 0 ml 0 ml 0 ml 5 mM 0 ml 0 ml 0 ml 10 mM 0 ml 0 ml 0 ml 50 mM 0 ml 0 ml 0 ml
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