[CAS NO. 1807988-47-1]  IITZ-01

Treatment with IITZ-01 results in the vacuolated appearance of cells due to its specific accumulation in lysosomes. It deacidifies lysosomes and inhibits maturation of lysosomal enzymes leading to lysosomal dysfunction. IITZ-01 enhances autophagosome accumulation but inhibit autophagosomal degradation by impairing lysosomal function, finally resulting in the inhibition of autophagy. It also abolishes mitochondrial membrane potential and triggered apoptosis through the mitochondria-mediated pathway. In in-vitro screening assays, IITZ-01 shows negligible inhibition toward PI3K γ (IC50: 2.62 μM) and no significant inhibition at 10 μM against mTORC1. Immunoblotting experiment has revealed no significant decrease in p-AKT levels in breast cancer cells when treated with IITZ-01. IITZ-01 can trigger apoptosis via disrupting MMP and modulating Bcl-2 and IAP family proteins.