Aurora kinase-IN-1, a potent aurora kinase inhibitor, modulates cell cycle progression and induces apoptosis by upregulating G1 cell cycle inhibitory proteins (including p21 and p27), elevating G1 progressive cyclin D1, and downregulating G1-to-S progressive cyclins, thereby arresting the cell cycle at the G1/S boundary. It stands as a promising lead compound for the development of chemotherapeutic agents.