化合物 T12819
| 中文名称 | 化合物 T12819 |
|---|---|
| 中文同义词 | 化合物 T12819 |
| 英文名称 | S130 |
| 英文同义词 | S130;7H-Dibenzo[de,g]quinoline-4-carboxamide, N-[3-(diethylamino)propyl]-7-oxo-;S130,S-130 |
| CAS号 | 1160852-22-1 |
| 分子式 | C24H25N3O2 |
| 分子量 | 387.47 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1160852-22-1.mol |
| 结构式 |  |
化合物 T12819 性质
| 沸点 | 641.5±50.0 °C(Predicted) |
|---|---|
| 密度 | 1?+-.0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | DMSO：125 mg/mL（322.61 mM；需要超声波） |
| 酸度系数(pKa) | 13.15±0.20(Predicted) |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
IC50: 3.24 µM (ATG4B)
S130 suppresses autophagy and activates apoptosis by inhibiting ATG4B, leads to enhanced cytotoxicity.
S130 (10 μM; 6 hours) suppresses autophagy at the early LC3 priming step or late autolysosome degradation stage.
S130 accumulates autolysosomes with more lipidated LC3.
S130 (0-25 μM; 48 hours) induces cell death through inhibiting the activity of ATG4B at a dose higher than 6.3 µM. And such cytotoxicity might not cause cell death through necroptosis.
Nutrient deprivation enhances S130-induced cytotoxicity.
S130 (0-10μM; 24 hours) suppresses approximately 79% of the cleavage of full-length LC3-GST at the 10 µM, while no substrates were processed in ATG4B KO cells. S130 displays obvious inhibitory effects on ATG4B.
Cell Cytotoxicity Assay
| Cell Line: | HeLa cells, HCT116 cells, HL60 cells |
| Concentration: | 0 μM, 3.1 μM, 6.3 μM, 12.5 μM, 25 μM |
| Incubation Time: | 48 hours |
| Result: | Had significant cytotoxic effects on HeLa cells (IC 50 =16.1 µM), HCT116 cells(IC 50 =9.0 µM) and HL60 cells (IC 50 =4.7 µM) at a dose higher than 6.3 µM. And such cytotoxicity might not cause cell death through necroptosis. |
Cell Autophagy Assay
| Cell Line: | HeLa cells and MEF cells |
| Concentration: | 10 μM |
| Incubation Time: | 6 hours |
| Result: | Suppressed autophagy at the early LC3 priming step or late autolysosome degradation stage. |
Western Blot Analysis
| Cell Line: | HeLa cells |
| Concentration: | 0 μM, 5 μM, 10 μM |
| Incubation Time: | 24 hours |
| Result: | Suppressed approximately 79% of the cleavage of full-length LC3-GST at 10 µM, while no substrates were processed in ATG4B KO cells. |
S130 (20 mg/kg; i.p.; daily; 3 weeks) suppresses tumor growth, and shows an efficient in vivo antitumor effect with a sound safety on vital organs.
| Animal Model: | BALB/c nude female mice (4 weeks), with HCT116 cells xenograft |
| Dosage: | 20 mg/kg |
| Administration: | Intraperitoneal injection; daily; 3 weeks |
| Result: | Was able to suppress tumor growth and with a sound safety on vital organs. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/08/19 | HY-112818 | S130 | 1 mg | 1590元 | |
| 2024/08/19 | HY-112818 | 暂无 S130 | 1160852-22-1 | 5mg | 3500元 |