Aminosulfonic acid and ammonium aminosulfonate were initially developed as herbicides. They are claimed to act as contact toxic agents when applied directly to plants, and exhibit a gametocidal effect when applied to the soil.

In the 1978 experiment on the gametocidal effect of aminosulfonic acid on rice conducted in Guangdong Province, China, its efficacy was better than that of other salts. Spraying at concentrations of 0.05% to 0.5% resulted in a gametocidal rate of 95% to 100%, but the efficacy was not stable enough and caused phytotoxicity. The typical herbicidal concentration of aminosulfonic acid is usually 75 g/L of active ingredient.