PI3K/AKT-IN-1 is a dual-acting inhibitor of PI3K/AKT pathway with an IC50 of 6.99 µM, 4.01 µM, and 3.36 µM, for PI3Kδ, PI3Kγ and AKT-1 respectively. It also induces S-phase cell cycle arrest, caspase-3-dependent apoptosis, exhibiting strong potential against breast cancer and leukemia.