Table 2.
Summary of known efflux inhibitor profile with potential fluorescent probes.
| Fluorescent substrate | Lasalocid | Loxapine | Mometasone | Nicardipine | Pimozide | Verapamil | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
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| B1 | C1 | G2 | B1 | C1 | G2 | B1 | C1 | G2 | B1 | C1 | G2 | B1 | C1 | G2 | B1 | C1 | G2 | |
| B22461c | – | – | w | – | – | – | 9.1 ± 8.4 | 3.7 ± 1.0 | 4.4 ± 3.4 | 3.2 ± 1.0 | 1.2 ± 0.9 | 4.3 ± 2.3 | w | 11.1 ± 6.4 | 14.2 ± 4.3 | w | 12.4 ± 4.9 | – |
| B7431a | – | – | – | 15.6 ± 10.9 | 10.1 ± 4.4 | – | 1.9 ± 1.1 | 1.6 ± 1.0 | – | 6.8 ± 4.8 | 2.6 ± 1.1 | – | 5.2 ± 5.2 | 9.7 ± 8.2 | – | 9.9 ± 6.6 | 12.3 ± 2.5 | – |
| B7433a | – | – | w | 15.9 ± 6.3 | 8.0 ± 1.9 | w | 2.6 ± 1.1 | 1.0 ± 0.5 | 2.1 ± 0.8 | 0.6 ± 0.3 | 2.6 ± 2.2 | 1.0 ± 0.8 | 9.4 ± 4.6 | w | W | 12.3 ± 7.4 | 7.2 ± 7.3 | – |
| B7469a | – | – | w | 4.3 ± 1.4 | w | w | 0.5 ± 0.1 | w | – | 2.0 ± 2.0 | 6.2 ± 6.0 | 0.7 ± 0.4 | 7.0 ± 1.9 | w | – | w | w | w |
| B7487a | – | – | – | 6.1 ± 2.3 | 15.5 ± 5.8 | – | 1.2 ± 1.3 | 1.0 ± 0.7 | – | 1.9 ± 2.3 | 0.6 ± 0.0 | – | w | w | – | 7.1 ± 6.2 | w | – |
| C1430b | – | – | – | w | w | – | 1.9 ± 1.6 | 5.4 ± 5.6 | – | 5.8 ± 2.8 | 4.3 ± 5.0 | – | 13.0 ± 3.0 | 7.7 ± 3.2 | – | w | w | – |
| C2927c | – | – | – | w | w | – | 0.8 ± 0.2 | w | – | 1.1 ± 0.8 | 0.6 ± 0.4 | – | 6.1 ± 1.3 | w | W | 17.9 ± 19.9 | 15.5 ± 6.7 | – |
| D14730a | – | – | – | 8.3 ± 6.5 | 12.9 ± 8.0 | – | 2.4 ± 1.6 | 1.4 ± 0.3 | – | 4.0 ± 2.1 | 5.3 ± 2.9 | – | 2.4 ± 1.3 | 1.9 ± 0.7 | – | 12.8 ± 1.9 | 5.8 ± 2.7 | – |
| D22421a | – | – | – | 1.7 ± 0.9 | 2.5 ± 1.7 | – | 0.9 ± 0.6 | 1.9 ± 1.4 | – | 0.6 ± 0.5 | 2.7 ± 4.1 | – | 3.5 ± 2.6 | 9.4 ± 3.6 | – | 1.5 ± 0.4 | 1.1 ± 0.3 | – |
| D2390c | 9.0 ± 6.2 | 13.5 ± 2.1 | 4.2 ± 2.4 | 9.8 ± 6.0 | w | w | 1.5 ± 0.6 | 2.5 ± 1.8 | w | 1.2 ± 0.9 | 1.0 ± 0.4 | w | 5.9 ± 1.9 | 3.7 ± 2.8 | – | 6.2 ± 5.3 | 9.6 ± 4.4 | – |
| D272a | – | – | – | w | w | – | 0.7 ± 0.2 | 2.1 ± 2.5 | – | 2.6 ± 3.8 | w | – | 3.8 ± 1.5 | 2.9 ± 0.7 | W | w | 22.1 ± 11.7 | – |
| D273a | – | – | – | w | w | – | 0.3 ± 0.1 | w | – | 0.8 ± 0.9 | w | – | 1.7 ± 0.9 | 1.4 ± 0.7 | W | 6.3 ± 7.3 | 7.1 ± 3.2 | – |
| D306c | – | – | – | 20.1 ± 19.4 | – | – | 3.2 ± 4.6 | 10.2 ± 9.3 | – | 1.4 ± 0.6 | – | – | 3.9 ± 3.2 | w | – | 8.0 ± 8.8 | w | – |
| E34251c | – | – | w | w | w | – | 2.7 ± 1.9 | w | – | 5.0 ± 1.5 | 4.0 ± 3.2 | – | w | 12.9 ± 9.1 | – | w | w | – |
| H14700a | w | w | – | w | w | – | 4.1 ± 2.5 | 3.9 ± 2.2 | – | 3.3 ± 2.5 | w | – | 10.8 ± 2.9 | 6.0 ± 2.1 | – | w | w | – |
| L7595c | – | – | – | 15.2 ± 7.5 | – | – | 0.9 ± 0.2 | w | – | 1.7 ± 1.0 | w | – | 7.1 ± 3.0 | – | – | 8.9 ± 5.7 | w | – |
| M7510c | – | – | – | w | w | – | 2.2 ± 1.6 | w | – | 2.0 ± 0.7 | w | – | 5.8 ± 3.4 | w | – | w | w | – |
| M7514c | – | – | – | 6.7 ± 0.1 | w | – | 6.6 ± 8.7 | 3.6 ± 0.9 | – | 7.8 ± 1.9 | 11.9 ± 10.8 | – | 7.8 ± 9.3 | w | – | 7.1 ± 1.1 | 11.1 ± 1.5 | – |
| R634a | – | – | – | w | – | – | 3.6 ± 2.2 | w | – | 10.1 ± 5.6 | w | – | w | w | – | w | – | – |
| R648MPc | w | – | – | w | – | – | 2.9 ± 2.0 | 2.2 ± 1.1 | – | 0.4 ± 0.2 | w | – | 5.3 ± 4.9 | 2.6 ± 2.3 | – | w | – | – |
| S34854a | – | – | – | w | w | – | 3.1 ± 2.5 | 1.2 ± 1.0 | – | 2.0 ± 0.6 | 5.6 ± 6.7 | – | 6.9 ± 1.3 | w | W | 23.1 ± 0.3 | 9.9 ± 0.2 | – |
| S7575a | – | – | – | 9.8 ± 3.1 | 16.2 ± 4.8 | – | 1.6 ± 1.6 | 1.0 ± 0.8 | – | 2.3 ± 1.1 | 1.4 ± 1.1 | – | 7.1 ± 4.5 | 7.2 ± 2.6 | – | 7.1 ± 1.9 | 15.3 ± 7.5 | – |
| S7578a | – | – | – | w | w | – | 0.6 ± 0.3 | w | – | 1.8 ± 2.6 | – | – | 8.3 ± 7.0 | 3.3 ± 0.4 | W | w | w | – |
| T3168c | – | – | 5.1 ± 3.9 | w | w | w | 2.6 ± 1.9 | 7.0 ± 3.6 | 0.9 ± 0.1 | 3.7 ± 0.8 | 2.6 ± 1.5 | 0.5 ± 0.1 | 15.6 ± 7.6 | 5.3 ± 2.6 | 5.7 ± 4.2 | w | w | – |
| T639c | – | – | – | w | w | – | 1.1 ± 0.4 | 3.6 ± 2.3 | – | 1.1 ± 0.5 | w | – | 4.6 ± 0.4 | 7.5 ± 2.7 | – | w | 16.7 ± 4.0 | – |
| T669c | – | – | – | – | – | – | 7.1 ± 8.2 | w | – | 9.4 ± 3.6 | w | – | w | – | – | – | – | – |
| V12390c | – | – | – | 22.3 ± 2.5 | w | – | 3.0 ± 2.6 | 1.8 ± 1.1 | – | 0.6 ± 0.4 | 1.8 ± 1.4 | – | w | w | – | 6.2 ± 0.2 | 9.2 ± 6.1 | – |
Note. B1, ABCB1-overexpressing CCRF-ADR 5000 cells; C1, ABCB1-overexpressing SupT1-Vin cells; G2, ABCG2-overexpressing Ig-MXP3 cells. Values are mean IC50 values ± standard deviations (n ≥ 2). The fluorescent substrate concentrations used were one of the following: a100 nM; b250 nM; c500 nM. A dash (–) indicates a lack of response, and a “w” indicates an apparent inhibitory response that fell outside of the tested concentration range or the established cutoff parameters.