Table 1.

Selected examples of classical BCRP inhibitors.

Inhibitor	Substrate	Cell Line	ATPase Activity	Photoaffinity Labeling	Specificity
FTC [14,15]	MX	S1-M1-3.2	Inhibited	XX	Yes
Novobiocin [16]	TPT	PC6/SN2-5H2	XX	XX	Yes
Elacridar [17,18,19]	MX	MCF-7 MX	Inhibited	Unaffected	No
Reserpine [20,21]	H33342	SP	XX	Inhibited	No
Cyclosporin A [22,23,24]	PhA, MX	HEK/482R	Inhibited	Unaffected	No
Tariquidar [25]	MX	H460/MX20	Stimulated	XX	No
Ortataxel [26]	MX	8226/MR20	Decreased	XX	No
Gefitinib [27]	H33342	PLB-ABCG2	Inhibited a	XX	No

MX: Mitoxantrone; PhA: Pheophorbide A; TPT: Topotecan; H33342: Hoechst 33342 dye; ^a: At high concentration; XX: Not yet reported.