Product Details
| Product Name:
AP-III-a4 |
CAS No.:
1177827-73-4 |
| Purity:
99.90% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| 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)
|
| 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 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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