Our present study revealed that 5,7-dihydroxyflavone is a potent sensitizer to TRAIL and the combination of 5,7-dihydroxyflavone and TRAIL is selectively active in cancer cells without affecting normal hepatocytes, indicating that the combination of 5,7-dihydroxyflavone and TRAIL may be an effective approach for the treatment of cancer. The gene discussed is TNFSF10; the disease is cancer.