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AP-III-a4

Name: AP-III-a4
Brand: TargetMol
SKU: T6759
Price: 47 USD
Availability: InStock
Rating: 4.5 (1 reviews)

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

Catalog No. T6759Cas No. 1177827-73-4

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Purity:99.90%

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COA HNMR HPLC

AP-III-a4

Catalog No. T6759Cas No. 1177827-73-4

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

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.

Pack Size	Price	Availability
1 mg	$47	In Stock
5 mg	$172	In Stock
10 mg	$278	In Stock
25 mg	$563	In Stock
50 mg	$786	In Stock
100 mg	$1,090	In Stock

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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.
Alias	ENOblock

Chemical Properties

Molecular Weight	594.72
Formula	C₃₁H₄₃FN₈O₃
Cas No.	1177827-73-4

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

Solubility Information

DMSO: 50 mg/mL (84.07 mM), Sonification is recommended.

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

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

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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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

Dose Conversion

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