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Aim: PAC-1 is the first small molecular compound identified to induce apoptosis by direct activation of procaspase-3 into caspase-3, the main executor of apoptosis.YCL-0426 is a potent procaspase-3 activating compound synthesized in our lab.In this study, the antitumor mechanism and the impact to other signal pathways of PAC-1 and YCL0426 were investigated.