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AP-III-a4

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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.

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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.
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

Solubility Information

DMSO: 30 mg/mL (47.53 mM)

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

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
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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