CA-5F

中文名称:

CA-5F

中文同义词:

化合物CA-5F

英文名称:

CA-5f

英文同义词:

CA-5f;CA-5F;CA 5F;CA5F;1370032-19-1;4-Piperidinone, 3-[(3,4-dimethoxyphenyl)methylene]-5-(1H-indol-3-ylmethylene)-1-methyl-, (3E,5E)-;-5-(1H-indol-3-ylmethylene)-1-methyl-, (3E,5E)-

CAS号:

1370032-19-1

分子式:

C24H24N2O3

分子量:

388.46

EINECS号:

相关类别:

API

Mol文件:

1370032-19-1.mol

生物活性

CA-5f 是一种有效的晚期巨自噬/自噬 (macroautophagy/autophagy) 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。具有抗肿瘤活性。

靶点

Macroautophagy/autophagy

体外研究

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. 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. CA-5f (20 μM) neither impairs the hydrolytic function nor the quantity of lysosomes. CA-5f (20 μM, 96 hours) inhibits the growth of A549 cells, and less cytotoxic to normal HUVECs. Cell Viability Assay 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 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.

Cell Line:

A549, HUVECs

Concentration:

20 μM

Incubation Time:

96 hours

Result:

Exhibited more cytotoxicity against A549 cells compared with normal HUVECs.

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.

体内研究

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. CA-5f (40 mg/kg, i.p.) suppresses autophagic flux and induces apoptosis in nude mice bearing A549 lung cancer cells. Animal Model: Nude mice bearing A549 lung cancer cells 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.

Animal Model:

Nude mice bearing A549 lung cancer cells

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.