Arsenic (As) is one of the most toxic contaminants to food crops, and as such, decreasing crops uptake and accumulation of As cannot be overemphasized. Here, we characterized a functional wheat NIP2;1 homolog of the As transporter, TaNIP2;1. TaNIP2;1 expression was suppressed by arsenite (As(III)) in wheat. Ectopic expression of TaNIP2;1 in the Δfps1 yeast mutant enhanced yeast sensitivity towards As(III). Conversely, the elevated expression of TaNIP2;1 in Δacr3 mutants decreased yeast sensitivity to arsenate (As(V)), demonstrating that TaNIP2;1 showed both influx and efflux transport activities for As(III) in yeasts. This is further supported by increased As concentration in the yeast cells that overproduce TaNIP2;1 in Δfps1, while As concentration decreased in Δacr3. Furthermore, ectopic expression of TaNIP2;1 in Arabidopsis confirmed that TaNIP2;1 can transport As into plants, as supported by increased sensitivity to and uptake of As(III). No change in plant sensitivity was found to Cu(II), Cd(II), Zn(II) or Ni(II), indicating that transport activity of TaNIP2;1 is specific for As(III). Taken together, our data show that TaNIP2;1 may be involved in As(III) transportation in plants. This finding reveals a functional gene that can be manipulated to reduce As content in wheat.