PURPOSE: A composition containing NADPH oxidase complex protein and/or diphenylene iodonium and/or derivative thereof is provided to treat and diagnose cancer. CONSTITUTION: A composition for preventing and treating cancer contains therapeutically effective amount of diphenylene iodonium, derivative thereof, or pharmaceutically acceptable salt thereof as an active ingredient. The therapeutically effective amount is 1mg/kg to 1000 mg/kg. The composition is administered by combining with an anti-cancer drug such as cisplatin, taxol, taxotere, doxorubicin, etoposide, gleevec, arimidex, tamoxifern, epirubicin, adriamycin, or valstar.본 발명은 암을 치료, 및 진단하기 위한 조성물 및 방법에 관한 것으로 더욱 상세하게는 NADPH 옥시데이즈 복합체 계열 단백질 및/또는 다이페닐렌아이오도니움, 및/또는 그 유도체를 유효성분으로 하는 암을 치료, 및 진단하기 위한 조성물에 관한 발명이다.