To specifically enhance pro-apoptotic effects of the caspase-8/c-FLIPL heterodimer in cancer cells we have rationally designed the small molecule termed FLIPinB/FLIPinBγ targeting caspase-8-p43/c-FLIPL heterodimer, the processed form of procaspase-8/c-FLIPL heterodimer25. The gene discussed is CASP8; the disease is cancer.