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Chronic ingestion of arsenic-contaminated drinking water induces skin lesions and urinary bladder cancer in humans. It is now recognized that thioarsenicals such as dimethylmonothioarsinic acid (DMMTA^V) are commonly excreted in the urine of humans and animals and that the production of DMMTA^V may be a risk factor for the development of the diseases caused by arsenic. The toxicity of DMMTA^V was compared with that of related nonthiolated arsenicals with respect to cell viability, uptake ability, generation of reactive oxygen species (ROS), and cell cycle progression of human epidermoid carcinoma A431 cells, arsenate (iAs^V), arsenite (iAs^III), dimethylarsinic acid (DMA^V), and dimethylarsinous acid (DMA^III) being used as reference nonthiolated arsenicals. DMMTA^V (LC₅₀ = 10.7 µM) was shown to be much more cytotoxic than iAs^V (LC₅₀ = 571 µM) and DMA^V (LC₅₀ = 843 µM), and its potency was shown …