1160852-22-1
1160852-22-1 結(jié)構(gòu)式
基本信息
S130,S-130
7H-Dibenzo[de,g]quinoline-4-carboxamide, N-[3-(diethylamino)propyl]-7-oxo-
物理化學(xué)性質(zhì)
常見(jiàn)問(wèn)題列表
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. |