After Feng Shao discovered that the activation of caspase-3 by chemotherapeutic agents could trigger pyroptosis by cleaving GSDME [113], numerous studies showed that small-molecule inhibitors or traditional chemotherapeutic drugs could cause cell death via pyroptosis when tumor-expressing GSDME was cleaved by activated caspase-3 in various cancers [87,88,89,92] (Table 2). Here, CASP3 is linked to cancer.