TABLE 3.
Efficacy of MCTs inhibitors.
| Inhibitor | Inhibition index | MCT1 | MCT2 | MCT4 | Other targets | Ref |
|---|---|---|---|---|---|---|
| Syrosingopine | IC50(um) | ∼ 2.5 | ND | ∼ 0.04 | vesicular monoamine | Benjamin et al. (2018) |
| CHC | IC50(um) | 150 | ND | ≥150 | mitochondrial pyruvate carrier | Jonnalagadda et al. (2019) |
| compounds 1–9 | IC50(um) | 0.008–0.048 | ND | 0.011–0.085 | — | Jonnalagadda et al. (2019) |
| phloretin | Ki(um) | 14 | 5 | 41 ± 8.8 (4) | glucose transporters | Manning Fox et al. (2000) |
| DIDS | Ki(um) | 434 | ND | NI | bicarbonate transporters | Manning Fox et al. (2000) |
| quercetin | IC50(um) | 14 ± 5 | 5 ± 2 | ND | ERβ | Bröer et al. (1999) |
| ARC155858 | Ki(nm) | 2.3 | ＜10 | NI | — | Ovens et al. (2010b) |
| AZD3965 | Ki(nm) | 1.6 | 9.6 | NI | — | Critchlow et al. (2012) |
| BAY-8002 | IC50 (nm) | 1 | 5 | >500 | — | Quanz et al. (2018) |
| 7ACC2 | IC50 (nm) | 11 | ND | ND | — | Draoui et al. (2014) |
Abbreviations:CHC: α-cyano-4-hydroxycinnamate; compounds 1–9: 2-methoxy-4-N,N-dialkyl cyanocinnamic acids 1–9; DIDS: 4,4′-diisothiocyanostilbene-2, 2′-disulphonate; ND, not determined; NI, no inhibition.