| 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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Cell Div, 2025, 20(1):23
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J Exp Clin Cancer Res, 2023, 42(1):1
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bioRxiv, 2023, 10.1101/2023.08.01.551011
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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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| E7903 |
Glucosylsphingosine
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Glucosylsphingosine (lyso-Gb1) is a deacylated form of glucosylceramide and is also degraded by the glucocerebrosidase. This compound is a very promising, reliable and specific biomarker for monitoring Gaucher disease.
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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 |
PFK15
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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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J Transl Med, 2024, 22(1):954
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bioRxiv, 2023, 10.1101/2023.08.01.551011
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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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bioRxiv, 2025, 2025.05.25.655979
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Life Med, 2023, 2(1):lnad006
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Nat Metab, 2022, 4(10):1287-1305
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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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Mol Cell Proteomics, 2023, 22(11):100649
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Mol Cell Proteomics, 2023, 10.1016/j.mcpro.2023.100649
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Research Square, 2023, Version 1
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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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Mol Med Rep, 2019, 19(4):2921-2926
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| S6496 |
Genz-123346 free base
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Genz-123346 is an inhibitor of GL1 synthase that blocks the conversion of ceramide to GL1, the first step in the biosynthesis of gangliosides and other glycosphingolipids.
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