ENOblock (AP-III-a4) is a unique small molecule inhibitor of the glycolysis enzyme Enolase with IC50 of 576 nM, binds enolase and modulates its non-glycolytic functions.
ENOblock induces enolase nuclear localization and modulates target gene expression in both hepatocytes and adipocytes.
ENOblock (12 mg/kg) reduces blood glucose, LDL cholesterol and enolase activity, also reduces the serum level of free fatty acid (FFA) in T2DM mice, without liver hepatocyte toxicity.
ENOblock reduces liver fibrosis and apoptosis in T2DM mice, inhibits the expression of inflammatory markers and key regulators of lipid homeostasis and gluconeogenesis in the T2DM liver.
ENOblock reduces cardiac hypertrophy, fibrosis, apoptosis and pathological markers in T2DM mice.
ENOblock significantly inhibits cancer cell invasion of HCT116 cancer cells at 625 nM, decreases the expression of AKT and Bcl-xL.
ENOblock can inhibit cancer cell metastasis in vivo.