Name | CA-5f |
Description | CA-5f is a potent late-stage macroautophagy/autophagy inhibitor that works by inhibiting autophagosome-lysosome fusion. |
Cell Research | 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. |
Animal Research | 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. |
In vitro | 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. |
In vivo | 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. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 55 mg/mL (141.58 mM) H2O : Insoluble
|
Keywords | Apoptosis | inhibit | Autophagy | Inhibitor | CA-5f | CA 5f | CA5f |
Inhibitors Related | Stavudine | 5-Fluorouracil | Sodium 4-phenylbutyrate | L-Ascorbic acid | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Tributyrin | Curcumin | Paeonol | Naringin | Gefitinib |
Related Compound Libraries | Apoptosis Compound Library | Bioactive Compound Library | Autophagy Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |