P-gp, the product of the MDR gene MDR1, and MRPs are members of the superfamiliy of ABC transporters. They are localized in the luminal membrane of endothelial cells and function to detoxify or eliminate a spectrum of harmful agents and chemicals by mediating energy-dependent transport from the cell. While their expression in normal cells protects the cells from xenobiotic attack, their expression in other cells, such as cancer cells, can be a significant obstacle to drug efficacy. Cayman's Multidrug Resistance Assay Kit provides a convenient tool for studying MDR protein modulators. The kit employs calcein AM, a substrate for MDR proteins including P-gp and MRP, as a probe for the detection of chemical compounds interacting with MDR proteins. Hoechst Dye is used as a marker of cell nuclei. Cyclosporin A, a competitive inhibitor, and verapamil, a noncompetitive inhibitor, are included as positive controls.