Human ABCG2 | Mouse ABCG2 | |||||
---|---|---|---|---|---|---|
H460 MX20 | MCF FLV500 | 3T3 MX15 | Ltk-HoeR415 | |||
Substrates | Conc. | Exc/Em | Effluxa ± S.D. (%) | |||
μM | ||||||
Mitoxantroneb | 10 | 630/660 | 78.3 ± 2.7 | 70.8 ± 1.5 | 69.9 ± 3.5 | 51.6 ± 4.5 |
Hoechst 33342b | 1 | 350/530 | 86.9 ± 2.3 | 67.6 ± 1.4 | 90.0 ± 6.5 | 52.9 ± 13.7 |
BODIPY-Prazosinb | 250 nM | 488/530 | 86.8 ± 1.3 | 77.4 ± 4.2 | 77.8 ± 3.2 | 70.4 ± 0.8 |
Pheophorbide a | 10 | 630/660 | 85.4 ± 0.6 | 80.9 ± 6.0 | 91.4 ± 0.8 | 46.0 ± 7.9 |
Pyropheophorbide a methyl ester | 10 | 630/660 | 90.1 ± 3.1 | 69.9 ± 1.0 | 80.5 ± 14 | 57.9 ± 12.2 |
Purpurin-18 | 15 | 630/660 | 92.5 ± 1.4 | 76.7 ± 1.0 | 67.3 ± 4.7 | 66.0 ± 10.4 |
Chlorin e6 | 50 | 630/660 | 84.7 ± 1.6 | 52.0 ± 5.0 | 72.2 ± 2.3 | 48.2 ± 5.5 |
Daunorubicinb | 1 | 488/570 | 13.1 ± 1.9 | 17.3 ± 2.9 | 18.6 ± 11.6 | 19.6 ± 11.6 |
Rhodamine123b | 2 | 488/530 | 0 | 0 | 21.3 ± 1.1c | 48.8 ± 2.3c |
↵a Accumulation is normalized to the fluorescence of cells in each substrate in the presence of Ko143 (10 μM) and the mean percentage difference with and without the inhibitor is recorded. Data represent means ± S.D. of three observations. Negative values were assigned the value of zero.
↵b Also substrates of P-gp.
↵c Due to baseline P-gp efflux.