Autophagy-IN-1 是一种有效的细胞自噬 (Autophagy) /线粒体自噬 (Mitophagy) 抑制剂，通过在阻断癌细胞内自噬体-溶酶体融合的同时选择性地增加自噬通量来发挥作用。Autophagy-IN-1 可诱导细胞凋亡 (Apoptosis) 和细胞周期阻滞。Autophagy-IN-1 在 HCT116 小鼠异种移植瘤模型中显著抑制肿瘤生长，且毒性低。Autophagy-IN-1 可用于结直肠癌的研究。

Autophagy-IN-1 is a potent autophagy / mitophagy inhibitor, acts by selectively increasing the autophagic flux while blocking the autophagosome-lysosome fusion in cancer cells. Autophagy-IN-1 can induce apoptosis and cell cycle arrest. Autophagy-IN-1 significantly inhibits tumor growth in an HCT116 xenograft mouse model and with low toxicity. Autophagy-IN-1 can be used for researching colorectal cancer [1].

Autophagy-IN-1 (compound 6) (1 and 5 μM; 8 h) induces apoptosis of HCT116 cells concentration-dependently [1]. Autophagy-IN-1 (0.5, 1, 5 and 10 μM; 6 h) decreases pro-PARP1, pro-caspase 8 and pro-caspase 3; increases Cleaved-PARP1, Cleaved-caspase 8 and Cleaved-caspase 3 concentration-dependently [1]. Autophagy-IN-1 increases LC3B-II, p62, and LAMP1 in HCT116 and SW620 cells, and increases number of autophagic/mitophagic vacuoles in HCT116 cells [1]. Apoptosis Analysis [1] Cell Line: HCT116 cells Concentration: 1 and 5 μM Incubation Time: 8 h Result: Induced 10.11% and 33.52% apoptosis of HCT116 cells at 1 μM and 5 μM. Western Blot Analysis [1] Cell Line: HCT116 cells Concentration: 0.5, 1, 5 and 10 μM Incubation Time: 24 h Result: Decreased pro-PARP1, pro-caspase 8 and pro-caspase 3; increased Cleaved-PARP1, Cleaved-caspase 8 and Cleaved-caspase 3 concentration-dependently. Cell Autophagy Assay [1] Cell Line: HCT116, SW620, and NCM460 cells Concentration: 0.5, 1, 5 and 10 μM Incubation Time: 0, 1, 2, 4, 9, 12 and 24 h Result: Led to a time- and dose-dependent increase of the levels of LC3B-II, p62, and LAMP1 in HCT116 and SW620 cells, and increased number of autophagic/mitophagic vacuoles in HCT116 cells.

Autophagy-IN-1 (50 and 100 mg/kg; IP, daily for 15 days) significantly inhibits tumor growth in an HCT116 xenograft mouse model [1]. Animal Model: Male BALB/c nude mice [1] Dosage: 50 and 100 mg/kg Administration: IP, daily for 15 days Result: Significantly inhibited tumor growth and did not observe weight loss.

C23H25NO7

427.45

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years