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].
Autophagy-IN-1 (50 and 100 mg/kg; IP, daily for 15 days) significantly inhibits tumor growth in an HCT116 xenograft mouse model[1].
References:
[1]. Yang ST, et al. Development of Strigolactones as Novel Autophagy/Mitophagy Inhibitors against Colorectal Cancer Cells by Blocking the Autophagosome-Lysosome Fusion. J Med Chem. 2022 Jul 19.