List of information on LDHA inhibitors
| LDHA inhibitors | Competitive sites | LDHA (Ki value) | Shortcomings | References |
|---|---|---|---|---|
| Oxamate | Pyruvate | 136.3 μM | High polarity, low exocytosis across cell membranes, high dosing concentration | [71–75] |
| (R)-(–)-gossypol | NADH | 1.9 μM | Non-specific toxicity | [76–78, 84, 85] |
| FX11 | NADH | 8 μM | Not yet used in clinical trials | [76, 78] |
| Quinoline 3-sulfonamides | NADH | 4–6 nM | Low clearance in vivo | [88] |
| GF | Pyruvate | 5.46 μM | Possible inhibition of RNA synthesis rather than blockage of glycolysis | [89, 92] |
| NADH | 56 μM | |||
| NHI | Pyruvate, NADH | 8.9 μM | Novel inhibitors to be studied | [15, 93] |
| GNE-140 | NADH | - | Novel inhibitors to be studied | [96] |
GF: galloflavin. Ki: inhibition constant; -: no literature has demonstrated it