AP-III-a4

SKU: orb1300492

Description

ENOblock is a potent, first-in-class nonsubstrate analogue inhibitor of enolase, exhibiting an IC50 of 0.576 μM. It is widely used in biochemical and cancer metabolism research, with applications in both in vitro enzymatic assays and in vivo studies exploring tumor growth inhibition.

Research Area

Cell Biology, Metabolism Research

Key Properties

• CAS Number: 1177827-73-4
• MW: 594.72
• Purity: 99.90% (May vary between batches)
• Formula: C₃₁H₄₃FN₈O₃
• SMILES: NCCOCCOCCNC(=O)Cc1ccc(Nc2nc(NCC3CCCCC3)nc(NCc3ccc(F)cc3)n2)cc1
• Target: Glucokinase,Apoptosis
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (8.41 mM);DMSO:257.5 mg/mL (432.98 mM)

Bioactivity

• Target IC50:
  Enolase:0.576 μM
• 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.
• 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.
• 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.
• Animal Research:
  In HCT116-xenotransplanted zebrafish tumor xenograft model, were treated with AP-III-a4 of 10 μM.

Storage & Handling

• Storage: store at low temperature | Pure form: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Apoptosis, AP III a4, APIIIa4, AP-III-a4, AP-III-a-4, anticancer, antidiabetic, inhibit, Inhibitor, Huh7, enolase, Enolase, ENOblock, HEK, HCT116, zebrafish, Phosphopyruvate hydratase

Compound Identifiers

PubChem CID

24012277