AP-III-a4

SKU: orb1223408

Description

AP-III-a4 is the first, nonsubstrate inhibitor of enolase, blocking cancer cell metastasis in vivo.

Key Properties

• CAS Number: 1177827-73-4
• MW: 631.18
• Purity: >98% (HPLC)
• Formula: C₃₁H₄₄ClFN₈O₃
• SMILES: C1CCC(CC1)CNc1nc(nc(n1)NCc1ccc(cc1)F)Nc1ccc(cc1)CC(=O)NCCOCCOCCN
• Target: FAAH
• Solubility: In Vitro: DMSO : 100 mg/mL (168.15 mM)

Bioactivity

• In Vivo:
  AP-III-a4 (ENOblock) (10 μM; 96 h) inhibits cancer cell metastasis and suppresses the gluconeogenesis regulator PEPCK in zebrafish. Animal model: The zebrafish cancer cell HCT116 xenograft model. Dosage: 10 μM. Administration: 96 h. Result: Reduced cancer cell dissemination. Inhibited PEPCK expression and induced glucose uptake. Inhibited adipogenesis and foam cell formation.
• In Vitro:
  AP-III-a4 (ENOblock) (0-10 μM; 24 h) inhibits HCT116 cell viability in a dose-dependent manner. AP-III-a4 directly binds to enolase and inhibits its activity. AP-III-a4 (0-10 μM; 24 or 48 h) inhibits cancer cell migration and invasion, induces cancer cell apoptosis. AP-III-a4 (10 μM; 24 h) can induce glucose uptake and inhibit phosphoenolpyruvate carboxykinase (PEPCK) expression in hepatocytes and kidney cells. Cell Viability Assay Cell line: HCT116. Concentration: 1.25, 2.5, 5 and 10 μM Incubation time: 24 h. Result: Induced higher levels of HCT116 colon cancer cell death in hypoxic conditions compared to normoxia. Western blot analysis. Cell line: HCT116. Concentration: 1.25, 2.5, 5 and 10 μM Incubation time: 24 h for AKT, 48 h for Bcl-Xl. Result: Bound to enolase in cell lysate and bound to purified enolase. Decreased the expression of AKT and Bcl-Xl, which are negative regulators of apoptosis. Cell Invasion Assay Cell line: HCT116. Concentration: 0.156, 0.312, 0.625, 1.25 and 2.5 μM Incubation time: 24 h. Result: Significantly inhibits cancer cell invasion at a treatment concentration of 0.625 μM. Cell Migration Assay Cell line: HCT116. Concentration: 0.625, 1.25 and 2.5 μM Incubation time: 24 h. Result: Inhibited cell migration dose-dependently. RT-PCR Cell line: Huh7 and HEK. Concentration: 10 μM. Incubation time: 24 h. Result: Induced glucose uptake and inhibited PEPCK expression.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AP-III-a4

Quick Database Links

Gene Symbol

FAAH