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AdipoGen Life Sciences
AP-III-a4 . hydrochloride
90
CHF
CHF 90.00
In stock
AG-CR1-3696-M0011 mgCHF 90.00
AG-CR1-3696-M0055 mgCHF 360.00
| Product Details | |
|---|---|
| Synonyms | ENOblock |
| Product Type | Chemical |
| Properties | |
| Formula |
C31H43FN8O3 . HCl |
| MW | 594.7 . 36.5 |
| CAS | 1177827-73-4 (free base) |
| Purity Chemicals | ≥95% (HPLC) |
| Appearance | White to off-white solid. |
| Solubility | Soluble in DMSO (20mg/ml), ethanol (20mg/ml) or water (20mg/ml). |
| Identity | Determined by 1H-NMR. |
| InChi Key | UYGRNXLHKIBHMM-UHFFFAOYSA-N |
| Smiles | FC(C=C1)=CC=C1CNC2=NC(NC3=CC=C(CC(NCCOCCOCCN)=O)C=C3)=NC(NCC4CCCCC4)=N2.Cl |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice | Keep cool and dry. |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- Cell permeable first non-substrate analog enolase inhibitor (IC50=0.576µM). A recent study suggested no direct blocking of enolase activity in vitro and a indirect mechanism.
- Useful agent for immunometabolism research. The glycolysis enzymes enolase is known to have additional, non-glycolytic roles in cellular physiology, which has been termed 'moonlighting'.
- Anticancer agent. Inhibits cancer cell metastasis in a zebrafish cancer cell xenograft model. Induces cell death under hypoxia and inhibits cancer cell migration and invasion by down-regulation of AKT and Bcl-xL expression.
- Antidiabetic agent. Reduced hyperglycemia and hyperlipidemia in mice. Reduced blood glucose, LDL cholesterol and enolase activity in T2DM mice. Had beneficial effects on lipid homeostasis, fibrosis, inflammatory markers, nephrotoxicity and cardiac hypertrophy. Down-regulates phosphoenolpyruvate carboxykinase and sterol regulatory element-binding protein-1, which are known to produce anti-diabetic effects. Induced glucose uptake and inhibited phosphoenolpyruvate carboxykinase (PEPCK) expression in vitro.
- Reduced neuron-specific enolase (NSE) levels and suppressed neuroinflammation in an acute spinal cord injury (SCI) model.
Product References
- A unique small molecule inhibitor of enolase clarifies its role in fundamental biological processes: D.W. Jung, et al.; ACS Chem. Biol. 8, 1271 (2013)
- ENOblock Does Not Inhibit the Activity of the Glycolytic Enzyme Enolase: N. Satani, et al.; PLoS One 11, e0168739 (2016)
- ENOblock, a unique small molecule inhibitor of the non-glycolytic functions of enolase, alleviates the symptoms of type 2 diabetes: H. Cho, et al.; Sci. Rep. 7, 44186 (2017)
- Targeting Enolase in Reducing Secondary Damage in Acute Spinal Cord Injury in Rats: A. Haque, et al.; Neurochem. Res. 42, 2777 (2017)