The syntheses of novel glutathione derivatives as photoaffinity and fluorescent biochemical probes for the GS-X pump are described. GIF-0017, an S-alkylated glutathione derivative with a benzophenone photophore, competitively inhibits the transport of leukotriene C4 by the GS-X pump with an IC50 value of 0.40 μM, indicating the existence of strong interaction between the probe molecule and the GS-X pump.