| S7443 |
AP-III-a4 (ENOblock)
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AP-III-a4 (ENOblock) is the first nonsubstrate analogue inhibitor of enolase with IC50 of 0.576 μM.
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International Journal of Molecular Sciences, 2025, 8340
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Cell Division, 2025, 23
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Cell Div, 2025, 20(1):23
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| E1703 |
SF2312
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SF2312 is a highly potent inhibitor of Enolase with IC50s of 37.9 nM and 42.5 nM for human recombinant ENO1 and ENO2, respectively, and also is a natural phosphonate antibiotic. SF2312 displays activity against bacteria under anaerobic conditions.
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| E1028 |
POMHEX
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POMHEX, is a potent ENO2 -specific inhibitor of enolase and a racemic mixture, a cell-permeable pivaloyloxymethyl (POM) prodrug of HEX. It is also glycolysis inhibitor and can be used for the research of cancer.
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| S7289 |
PFK-015
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PFK15 (PFK-015) is a potent and selective 6-phosphofructo-2-kinase (PFKFB3) inhibitor with IC50 of 207 nM.
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Nature, 2025, 10.1038/s41586-025-09328-w
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Adv Healthc Mater, 2025, e2501417.
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Cell Commun Signal, 2025, 23(1):104
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| S7639 |
3PO
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3PO (3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one) is a small-molecule inhibitor of PFKFB3 with an IC50 of 22.9 μM for recombinant human PFKFB3 protein and does not inhibit PFK-1 activity. It suppresses glucose uptake, and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+, and NADH.
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Atherosclerosis, 2025, 405:119223
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bioRxiv, 2025, nan
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J Transl Med, 2024, 22(1):954
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| S8807 |
PFK158
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PFK158 is a potent and selective inhibitor of PFKFB3. It has improved PK properties and causes ~80% growth inhibition in several mouse models of human-derived tumors.
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Cancer & Metabolism, September 23, 2021, 33
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eLife, September 09, 2025, 107536
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Frontiers in Cellular and Infection Microbiology, October 08, 2025, 1648576
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| S6921 |
Dorzagliatin
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Dorzagliatin (HMS-5552, RO-5305552, Sinogliatin) is a dual-acting glucokinase (GK) activator that improves glycaemic control and pancreatic β-cell function in patients with type 2 diabetes.
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Pharmaceuticals (Basel), 2025, 18(6)927
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bioRxiv, 2025, 2025.04.03.647023
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bioRxiv, 2025, 2023.08.11.552890
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| S1830 |
Oxfendazole
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Oxfendazole (RS-8858,Fenbendazole sulfoxide) is a broad spectrum benzimidazole anthelmintic.
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bioRxiv, 2023, 2023.07.12.548707
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Nature Cell Biology, 2019, 203-213
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Molecular Medicine Reports, 2019, 2921-2926
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| S0400 |
KAN0438757
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KAN0438757 is a potent and selective inhibitor of the metabolic kinase PFKFB3 (6-Phosphofructo-2-Kinase/Fructose-2,6-Biphosphatase 3) with IC50 of 0.19 μM and 3.6 μM for PFKFB3 and PFKFB4, respectively.
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Current Issues in Molecular Biology, 2025, 892
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Molecular & Cellular Proteomics, 2023, 100649
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Mol Cell Proteomics, 2023, 22(11):100649
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| S2155 |
LY2608204
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LY2608204 activates glucokinase (GK) with EC50 of 42 nM. Phase 2.
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Scientific Reports, 2017, 44681
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Sci Rep, 2017, 7:44681
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Nat Commun, 2016, 7:11463
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