Enolase | Biologically Active Compounds

Enolase (phosphopyruvate hydratase) is a metalloenzyme responsible for the catalysis of the conversion of 2-phosphoglycerate (2-PG) tophosphoenolpyruvate (PEP), the ninth and penultimate step of glycolysis. Enolase belongs to the class Lyase. Enolase can also catalyze the reverse reaction, depending on environmental concentrations of substrates. The optimum pH for this enzyme is 6.5. Enolase is present in all tissues and organisms capable of glycolysis or fermentation. Small-molecule inhibitors of enolase have been synthesized as chemical probes of the catalytic mechanism of the enzyme. The most potent of inhibitors is phosphonoacetohydroxamate, which in its unprotonated form has pM affinity for the enzyme. It has structural similarity to the presumed catalytic intermediate, between PEP and 2-PG. Attempts have been made to use this inhibitor as an anti-trypanosome drug, and more recently, as an anti-cancer agent.

SF 2312

SF2312, a natural phosphonate Antibiotic (Antibiotic), is a highly potent Enolase (Enolase) inhibitor with IC50s of 37.9 nM and 42.5 nM for human recombinant ENO1 and ENO2, respectively. SF2312 is active against bacteria under anaerobic conditions[1].

CAS Number: 107729-45-3
MF: C₄H₈NO₆P
MW: 197.08300
Catalog: Bacterial

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D-(-)-3-Phosphoglyceric acid disodium

D-(-)-3-Phosphoglyceric acid (3-Phospho-D-glyceric acid) disodium is an important intermediate in the enzyme-catalysed process of glycolysis. D-(-)-3-Phosphoglyceric acid disodium competitively inhibits yeast enolase[1][2].

CAS Number: 80731-10-8
MF: C₃H₅Na₂O₇P
MW: 230.02100
Catalog: Enolase

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AP-III-a4

ENOblock(AP-III-a4) is a novel small molecule which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity (IC50=0.576 uM); inhibit cancer cell metastasis in vivo.IC50 value: 0.576 uM [1]Target: enolaseEnolase is a component of the glycolysis pathway and a “moonlighting” protein, with important roles in diverse cellular processes that are not related to its function in glycolysis. However, small molecule tools to probe enolase function have been restricted to crystallography or enzymology. In this study, we report the discovery of the small molecule “ENOblock”, which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity. ENOblock was isolated by small molecule screening in a cancer cell assay to detect cytotoxic agents that function in hypoxic conditions, which has previously been shown to induce drug resistance. Further analysis revealed that ENOblock can inhibit cancer cell metastasis in vivo. Moreover, an unexpected role for enolase in glucose homeostasis was revealed by in vivo analysis. Thus, ENOblock is the first reported enolase inhibitor that is suitable for biological assays. This new chemical tool may also be suitable for further study as a cancer and diabetes drug candidate.A Unique Small Molecule Inhibitor of Enolase Clarifies Its Role in Fundamental Biological ProcessesBy Jung, Da-Woon; Kim, Woong-Hee; Park, Si-Hwan; Lee, Jinho; Kim, Jinmi; Su, Dongdong; Ha, Hyung-Ho; Chang, Young-Tae; Williams, Darren R. From ACS Chemical Biology (2013), 8(6), 1271-1282.

CAS Number: 1177827-73-4
MF: C₃₁H₄₃FN₈O₃
MW: 594.723
Catalog: Enolase

Density: 1.3±0.1 g/cm3
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