Caspase-3/7 activator 1 is an effective activator of Caspase-3/7 that exhibits tumor-selective, antiproliferative activity and high apoptosis (Apoptosis) induction capability.

Caspase-3/7 activator 1 (Compound 7a) exhibits inhibitory effects on Wi-38, Caco-2, and HepG-2 cells, with IC50 values of 11.195 µM, 0.088 µM, and 0.115 µM, respectively. At a concentration of 0.06 μM for 72 hours, it significantly downregulates the expression of the apoptosis inhibitor Bcl2 in Caco-2 cells, decreasing Bcl2 by 0.471-fold. Additionally, it does not significantly affect the morphology of Caco-2 and HepG-2 cells. When applied at 0.088 µM for 72 hours, Caspase-3/7 activator 1 has the potential to induce apoptosis in Caco-2 cells, with a total apoptotic cell count of 50.905%.