| Name | AP-III-a4 |
| Description | AP-III-a4 (ENOblock) (ENOblock) is the first nonsubstrate analogue inhibitor of enolase with IC50 of 0.576 μM. |
| Cell Research | HCT116 cells(3 x 10E5) are seeded in a 6 well plate. 24 h later, cells are treated with AP-III-a4 (5 μM) for 24hours. |
| Kinase Assay | Enolase activity assay is in the 2.0 mM MgSO4 and 400 mM KCl in the absence or presence of ENOblock or NaF, at 37°C by incubating pure enolase (3–9 U) in a buffer containing 50 mM imidazole-HCl (pH 6.8). The reaction is initiated by adding 1 μmol of 2-phospho-D-glycerate, and the OD is measured after 10 min of reaction time with a spectrophometer at 240 nm. |
| Animal Research | In HCT116-xenotransplanted zebrafish tumor xenograft model, were treated with AP-III-a4 of 10 μM. |
| In vitro | AP-III-a4 induces glucose uptake and inhibits phosphoenolpyruvate carboxykinase (PEPCK) expression in Huh7 hepatocytes and HEK kidney cells. AP-III-a4 induces cell death under hypoxia, and inhibits cancer cell migration and invasion by down-regulation of AKT and Bcl-xL expression in HCT116 cells. |
| In vivo | AP-III-a4 (10 μM) inhibits cancer cell migration and invasion processes in HCT116-xenotransplanted zebrafish tumor model. In vivo, AP-III-a4 (10 μM) also inhibits adipogenesis and foam cell formation, and causes downregulation of PEPCK expression and induction of glucose uptake. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 50 mg/mL (84.07 mM), Sonification is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | Inhibitor | AP-III-a-4 | Phosphopyruvate hydratase | Apoptosis | inhibit | antidiabetic | anticancer | HCT116 | Enolase | Huh7 | zebrafish | APIIIa4 | HEK | AP-III-a4 | AP III a4 |
| Inhibitors Related | ARRY-403 | Globalagliatin | ML251 | PFK-015 | 3PO | PFKFB3-IN-2 | Oxfendazole | AZ PFKFB3 26 | AMG-1694 | PFK-158 | Dorzagliatin | PF-04937319 |
| Related Compound Libraries | Glycometabolism Compound Library | Glycolysis Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Inhibitor Library | NO PAINS Compound Library | Metabolism Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
