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AP-III-a4

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

(Synonyms: ENOblock) Copy Product Info

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Synonyms: ENOblock

Catalog No. T6759 Copy Product Info

Purity: 99.90%

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AP-III-a4 (ENOblock) is the first non-substrate analogue that directly binds to enolase to inhibit its catalytic activity with an IC50 of 0.576 μM, thereby blocking cancer cell metastasis in vivo. AP-III-a4 can be used in research on tumor metabolism, metastasis, and diseases related to carbohydrate metabolism.

Cas No. 1177827-73-4

Pack Size	Price	USA Stock	Global Stock
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

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.90%

Color:White

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COA HPLC HNMR

Product Introduction

Bioactivity

Description	AP-III-a4 (ENOblock) is the first non-substrate analogue that directly binds to enolase to inhibit its catalytic activity with an IC50 of 0.576 μM, thereby blocking cancer cell metastasis in vivo. AP-III-a4 can be used in research on tumor metabolism, metastasis, and diseases related to carbohydrate metabolism.
Targets & IC50	Enolase:0.576 μM
In vitro	Methods: H446 cells were treated with AP-III-a4 (1 μM) for 24 hours, followed by detection of ENO1 enzyme activity using the ENO1 Human Activity Assay Kit. Results: AP-III-a4 treatment inhibited ENO1 activity. [1]
In vivo	Methods: UM-1 cells (1×10⁶) were subcutaneously implanted into nude mice. Once tumor volume reached 100 mm³, AP-III-a4 was administered via intraperitoneal injection at a dose of 20 mg/kg body weight, every other day for 28 days. Results: Tumor volume and weight in AP-III-a4-treated mice were significantly smaller than in the control group. [2]
Synonyms	ENOblock
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.

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

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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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.