IITZ-01 is a cell penetrant and potent autophagy inhibitor in numerous cancer cells including breast, lung, and colon cancer cells. It significantly elevates LC3-II and SQSTM1 protein levels in starvation-induced autophagy conditions. IITZ-01 accumulates within lysosomes causing liposomal deacidification, impairment of lysosomal maturation and inhibition of lysosomal degradation. Additionally, IITZ-01 induces apoptosis through the mitochondria-mediated pathway in TNBC cells MDA-MB-231 and MDA-MB-453, while sparing normal mammary epithelial MCF10A cell.