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Indirubin is the active ingredient of a traditional Chinese herbal medicine, Danggui Longhui Wan, used for the treatment of chronic myelocytic leukemia. The author reports that novel indirubin derivative, 5'-nitro-indirubinoxime (5'-NIO), has potent anti-proliferative activity on human oral cancer cells. Treatment of KB cells with 5'-NIO showed a strong cell growth inhibition during indicated time point. A typical apoptosis pattern was obtained with DNA fragmentation and immunofluorescence analysis of anneixn-v-flous. Western blot data revealed that p53 and p21CIP1/Waf-1 level increased strongly upon 5'-NIO treatment. The author next tested whether 5'-NIO could activate apoptosis related proteins such as caspase-3/-7/-9. In cells exposed to 5'-NIO, activation of caspase-3 and -7 was observed. Interestingly, caspase-9 and cytochrome c could slightly activate in response to 5'-NIO. These results indicate that 5'-NIO strongly induces oral cancer cells apoptosis via a Mitochondria-mediated caspase cascade pathway. These observations together suggest that 5'-NIO may have a possible therapeutic potential to oral cancer.