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AP-III-a4

Name: AP-III-a4
Brand: TargetMol
SKU: T6759
Price: 47 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T6759Cas No. 1177827-73-4

Alias ENOblock

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

AP-III-a4

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Purity: 99.90%

Catalog No. T6759Alias ENOblockCas No. 1177827-73-4

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

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$47	In Stock	In Stock
2 mg	$71	In Stock	In Stock
5 mg	$123	In Stock	In Stock
10 mg	$198	In Stock	In Stock
25 mg	$388	In Stock	In Stock
50 mg	$619	In Stock	In Stock
100 mg	$987	In Stock	In Stock
200 mg	$1,450	-	In Stock
1 mL x 10 mM (in DMSO)	$159	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.90%

Color:White

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COA HPLC HNMR

Product Introduction

Bioactivity

Description	AP-III-a4 (ENOblock) (ENOblock) is the first nonsubstrate analogue inhibitor of enolase with IC50 of 0.576 μM.
Targets&IC50	Enolase:0.576 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.
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.
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.
Synonyms	ENOblock

Chemical Properties

Molecular Weight	594.72
Formula	C₃₁H₄₃FN₈O₃
Cas No.	1177827-73-4
Smiles	NCCOCCOCCNC(=O)Cc1ccc(Nc2nc(NCC3CCCCC3)nc(NCc3ccc(F)cc3)n2)cc1
Relative Density.	1.250 g/cm3 (Predicted)

Storage & Solubility Information

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.

Solubility Information

DMSO: 257.5 mg/mL (432.98 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (8.41 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.6815 mL	8.4073 mL	16.8146 mL	84.0732 mL
5 mM	0.3363 mL	1.6815 mL	3.3629 mL	16.8146 mL
10 mM	0.1681 mL	0.8407 mL	1.6815 mL	8.4073 mL
20 mM	0.0841 mL	0.4204 mL	0.8407 mL	4.2037 mL
50 mM	0.0336 mL	0.1681 mL	0.3363 mL	1.6815 mL
100 mM	0.0168 mL	0.0841 mL	0.1681 mL	0.8407 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc