Inhibitor | Concentration(s) Used in Present Study | Affected ABC Transporter(s) | Effect Reported in Literature | Reference(s) |
---|---|---|---|---|
μM | ||||
Cyclosporin A | 10 | Pgp, MRP1, and BCRP | 2.5 μM inhibited mitoxantrone efflux in Pgp-, MRP1-, and BCRP-overexpressing cell lines. | Qadir et al., 2005; Pawarode et al., 2007 |
GF120918 | 1, 5, and 10 | BCRP and Pgp | 25 to 250 nM inhibited rhodamine efflux in Pgp-overexpressing cells, and 1 to 10 μM inhibited mitoxantrone efflux in BCRP-overexpressing cells. | De Bruin et al., 1999 |
Ko143 | 1, 2, and 5 | BCRP | EC90 values of 23 and 26 nM for inhibiting mitoxantrone and topotecan efflux, respectively, in Bcrp1-overexpressing cells. | Allen et al., 2002 |
MK571 | 2.4 and 24 | MRP1/MRP2 | Inhibited leukotriene C4 transport in MRP-overexpressing cells with a Ki of 0.6 and 30 μM completely inhibited vincristine efflux in MRP-overexpressing cells. | Leier et al., 1994; Gekeler et al., 1995 |
PSC-833 | 5 | Pgp, MRPs | 2.5 μM inhibited mitoxantrone efflux in Pgp-overexpressing cells. | Qadir et al., 2005; Pawarode et al., 2007 |