AP-III-a4 (ENOblock)

For research use only.

Catalog No.S7443

4 publications

AP-III-a4 (ENOblock) Chemical Structure

CAS No. 2070014-95-6

AP-III-a4 (ENOblock) is the first nonsubstrate analogue inhibitor of enolase with IC50 of 0.576 μM.

Selleck's AP-III-a4 (ENOblock) has been cited by 4 publications

Purity & Quality Control

Biological Activity

Description AP-III-a4 (ENOblock) is the first nonsubstrate analogue inhibitor of enolase with IC50 of 0.576 μM.
Targets
enolase [1]
(Cell-free assay)
0.576 μM
In vitro

In HCT116 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 Huh7 hepatocytes and HEK kidney cells, AP-III-a4 induces glucose uptake and inhibits phosphoenolpyruvate carboxykinase (PEPCK) expression. [1]

Assay
Methods Test Index PMID
Western blot
p-AMPKα / AMPKα / p-ACC / ACC ; 

PubMed: 30242159     


Normal PASMC were treated with 10 μM ENOblock and hypoxia for 8 h, and the levels of p-AMPKα, AMPKα, p-ACC, and ACC were measured by western blotting in cell lysates. 

p-AKT / AKT / p-GSK3β / GSK3β / p-PRAS40 / PRAS40 ; 

PubMed: 30242159     


Normal PASMCs were treated with 10 μM ENOblock and hypoxia for 8 h, and the levels of p-Akt, pan-Akt, p-PRAS40, PRAS40, p-GSK3β, and GSK3β were measured by western blotting.

30242159
In vivo In a HCT116-xenotransplanted zebrafish tumor xenograft model, AP-III-a4 (10 μM) inhibits cancer cell migration and invasion processes. In vivo, AP-III-a4 (10 μM) also causes downregulation of PEPCK expression and induction of glucose uptake, and inhibits adipogenesis and foam cell formation. [1]

Protocol

Kinase Assay:

[1]

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Enolase activity assay:

A single unit of enolase is defined as the amount of enzyme that produces 1 μmol of phosphoenol pyruvate from phospho-D-glycerate/min in standard assay. Enolase activity assay is measured at 37°C by incubating pure enolase (3–9 U) in a buffer containing 50 mM imidazole-HCl (pH 6.8), 2.0 mM MgSO4 and 400 mM KCl in the absence or presence of ENOblock or NaF. 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.
Cell Research:

[1]

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  • Cell lines: HCT116 cells
  • Concentrations: 5 μM
  • Incubation Time: 24 h
  • Method:

    3 x 105 HCT116 cells are seeded in a 6 well plate. 24 h later, cells are treated with compound of interest (with or without prior induction of hypoxia for 4 h) for 24 h using triplicate wells. Cells are then trypsinized and resuspended in 2.5 mL PBS. A 100 μL aliquot is taken for staining with 0.2% trypan blue solution and counted using a hemocytometer. 150 cells are counted and dead cells are classified as those that could not exclude trypan blue.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: HCT116-xenotransplanted zebrafish tumor xenograft model
  • Dosages: 10 μM
  • Administration: --
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (158.43 mM)
Ethanol 100 mg/mL (158.43 mM)
Water 9 mg/mL (14.25 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 631.18
Formula

C31H44ClFN8O3

CAS No. 2070014-95-6
Storage powder
in solvent
Synonyms N/A
Smiles C1CCC(CC1)CNC2=NC(=NC(=N2)NCC3=CC=C(C=C3)F)NC4=CC=C(C=C4)CC(=O)NCCOCCOCCN.Cl

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID