Table 4. . Tricarboxylic acid cycle inhibitors.
Inhibitor | Target | IC50 | |
---|---|---|---|
Protein | Cell | ||
22 | MDH1/2 | 1–5 μM | 1–20 μM |
23 | mIDH | <50 nM | <50 nM |
24 | mIDH | <100 nM | N.D.R. |
25 | mIDH | <100 nM | N.D.R. |
26 | mIDH | <100 nM | <100 nM |
27 | mIDH | <10 nM | <10 nM |
28 | mIDH | <10 nM | <100 nM |
29 | mIDH | <100 nM | <10 nM |
30 | mIDH | 0.6 nM | N.D.R. |
31 | mIDH | 536 nM | N.D.R. |
32 | mIDH | 1–2 nM | N.D.R. |
33 | mIDH | 12 nM | 8 nM |
34 | mIDH | <20 nM | 6.7 nM |
35 | mIDH | 5.7 nM | 0.2 nM |
36 | mIDH | 3 nM | N.D.R. |
37 | mIDH | <300 nM | N.D.R. |
38 | mIDH | 7 nM | ∼20 nM |
39 | mIDH | <10 μM | ∼20 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. For values marked as ‘N.D.R.’, no data were reported for that compound. ‘Protein’ IC50 values were generally determined in systems with recombinant or otherwise purified proteins, while ‘Cell’ IC50 values generally apply to the inhibition of cancer cell growth, or a similar cellular readout.
MDH: Malate dehydrogenase; mIDH: Mutant isocitrate dehydrogenase.