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  • CA-5f
CA-5f的可视化放大

CA-5f

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。 CA-5f 增加 LC3B-II(一种监测自噬的标志物)和 SQSTM1 蛋白,并且还增加 ROS 的产生。抗肿瘤活性。

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CA-5f的二维码
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  • 货号: ajce50678
  • CAS: 1370032-19-1
  • 别名:
  • 分子式: C24H24N2O3
  • 分子量: 388.46
  • 纯度: >98%
  • 溶解度: DMSO : 77.5 mg/mL (199.51 mM);Water : < 0.1 mg/mL (insoluble)
  • 储存: Store at -20°C
  • 库存: 现货

Background

CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion. CA-5f increases LC3B-II (a marker to monitor autophagy) and SQSTM1 protein both in A549 cells and HUVECs. Anti-tumor activity[1].


CA-5f (0-40 μM, 6 hour) concentration- and time-dependently elevates the level of LC3B-II (a marker to monitor autophagy) and SQSTM1 protein both in A549 cells and HUVECs[1].CA-5f (20 μM, 6 hours) inhibits the degradation of autophagosomes when treated alone or in combination Bafilomycin A1 (100 nM) or Chloroquine (30 μM) in A549 cells and HUVECs[1].CA-5f (20 μM) neither impairs the hydrolytic function nor the quantity of lysosomes[1].CA-5f (20 μM, 96 hours) inhibits the growth of A549 cells, and less cytotoxic to normal HUVECs[1].|| Cell Viability Assay[1]||Cell Line:|A549, HUVECs|Concentration:|20 μM|Incubation Time:|96 hours|Result:|Exhibited more cytotoxicity against A549 cells compared with normal HUVECs.|| Western Blot Analysis[1]||Cell Line:|A549 cells and HUVECs|Concentration:|0-40 μM|Incubation Time:|6 hours|Result:|Elevated LC3B-II (a marker to monitor autophagy) and SQSTM1 protein levels in a concentration- and time-dependent manner.


CA-5f (40 mg/kg, i.p., every 2 days for up to 30 days) is well tolerated, and potently inhibits the growth of tumor in nude mice bearing A549 lung cancer cells[1]. CA-5f (40 mg/kg, i.p.) suppresses autophagic flux and induces apoptosis in nude mice bearing A549 lung cancer cells[1].|| Animal Model:|Nude mice bearing A549 lung cancer cells[1]|Dosage:|40 mg/kg|Administration:|Injected via caudal vein, every 2 days for up to 30 days|Result:|Significantly suppressed tumor volume and weight in mice, increased the number of apoptotic cells in mice.


[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.

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