Table 5. . Nutrient import inhibitors.
Inhibitor | Target | IC50 | |
---|---|---|---|
Protein | Cell | ||
40 | GLUT5 | 100 μM | N.D.R. |
41 | GLUT4 | 18.2 μM | 13.4 μM |
42 | GLUT1 | 25–40 nM | 80–700 nM |
43 | GLUT1 | ∼3 μM | 1–8 μM |
44 | GLUT1 | 336 nM | N.D.R. |
45 | GLUT1 | 37 nM | N.D.R. |
46 | LAT1 | 36–131 μM | 110 nM |
47 | ASCT2 | 240–310 nM† | N.D.R. |
48 | ASCT2 | 9.6 μM | ∼10–50 μM |
Summary of inhibitory potencies of compounds inhibiting steps in the tricarboxylic acid cycle. Values marked as approximate (∼) were generally read off a graph, while exact values were generally reported in a table.
Reported as a Ki rather than an IC50. For values marked as ‘N.D.R.’, no data were reported for that compound. ‘Protein’ IC50 values were generally determined against the ability of the transmembrane protein to transport its target molecule into a cell, while ‘Cell’ IC50 values generally apply to the inhibition of cancer cell growth, or a similar cellular readout.