Table 2.
PFKFB inhibitors.
| Inhibitors | Targets | Diseases | Developmental stage | References |
|---|---|---|---|---|
| 3PO | PFKFB3 | Jurkat T cell leukemia cells, breast cancer cells | In vitro study | [116], [137] |
| PFK-15 | PFKFB3 | Liver cancer, colon cancer, bladder cancer cells, CML | In vitro and preclinical evaluation | [118], [122] |
| PFK-158 | PFKFB3 | Hepatic metastatic tumor | Pharmacokinetic profiling, phase 1 clinical trial | [123] |
| N4A | PFKFB3 | HeLa cells | In vitro study | [138] |
| YN1 | PFKFB3 | HeLa cells | In vitro study | [138] |
| YZ9 | PFKFB3 | Not tested | Preliminary in vitro characterization | [138] |
| BrAcNHEtOP | Liver PFK2, testis PFK2 | Not tested | In vitro study | [139] |
| PQP | PFKFB3 | Colonic and bladder cancer cells | In vitro study; less growth inhibitory effect than PFK-15 | [122] |
| Compound 26 | PFKFB3 | Not tested | In vivo pharmacokinetic characterization | [140] |
| 5MPN | PFKFB4 | Lung adenocarcinoma cells | In vitro study, xenograft tumor | [124] |
Abbreviations: BrAcNHEtOP: N-bromoacetylethanolamine phosphate; 5MPN: 5-(n-(8-methoxy-4-quinolyl) amino) pentyl nitrate.