| CAS |
No.1370032-19-1 |
| 英文名称 |
CA-5f |
| 分子式 |
C24H24N2O3 |
| 分子量 |
388.46 |
| 溶解性 |
Soluble in DMSO |
| 纯度 |
≥98% |
| 外观(性状) |
Light yellow to yellow Solid |
| 储存条件 |
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL |
MFCD31813689 |
| SMILES |
O=C(/C(CN(C)C/1)=C/C2=CNC3=C2C=CC=C3)C1=C\C4=CC=C(OC)C(OC)=C4 |
| 靶点 |
Autophagy |
| 通路 |
Autophagy |
| 背景说明 |
CA-5f 是一种有效的晚期巨自噬/自噬抑制剂，通过抑制自噬体-溶酶体融合起作用。CA-5f 能够增加 LC3B-II (一种监控自噬的标记物) 和 SQSTM1 蛋白水平，促进 ROS 的产生。 |
| 生物活性 |
CA-5f是一种有效的自噬晚期（late-stage autophagy）抑制剂，通过抑制自噬体-溶酶体融合发挥作用。[1] |
| In Vitro |
CA-5f neither impairs the hydrolytic function nor the quantity of lysosomes. Treatment of human umbilical vein endothelial cells(HUVECs)with CA-5f for 1 h suppresses the levels of cytoskeletal proteins and membrane traffic proteins. CA-5f exhibits strong cytotoxicity against A549 non-small cell lung cancer(NSCLC)cells，but low cytotoxicity to normal human umbilical vein endothelial cells(HUVECs)，by increasing mitochondrial-derived reactive oxygen species(ROS)production. CA-5f inhibits autophagic flux by blocking autophagosome-lysosome fusion instead of affecting the pH and hydrolytic function of lysosomes[1]. |
| In Vivo |
CA-5f effectively suppresses the growth of A549 lung cancer xenograft as a single agent with an excellent tolerance in vivo. It inhibits autophagic flux，induced apoptosis，and does not affect the level of CTSB(cathepsin B)and CTSD(cathepsin D)in vivo[1]. |
| 细胞实验 |
A549 cells or HUVECs are seeded into E-Plate 16-well plates overnight and then treated with DMSO or CA-5f and continuously monitored for 96 h. The changes of cell index can be used to monitor cell viability.[1] |
| 动物实验 |
Animal Models: Four-week-old BALB/c nude mice(subcutaneous injection of A549 cells at the right scapula); Dosages: 40 mg/kg; Administration: injected via caudal vein[1] |
| 数据来源文献 |
[1] Zhang L， et al. Autophagy. 2019， 15(3):391-406. |
| 规格 |
1mg 5mg 10mg 25mg 50mg |
| 单位 |
瓶 |
中文
英语
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