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AP-III-a4

Catalog No. T6759 CAS 1177827-73-4

Synonyms: ENOblock

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

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AP-III-a4, CAS 1177827-73-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 47.00
5 mg	In stock	$ 172.00
10 mg	In stock	$ 278.00
25 mg	In stock	$ 563.00
50 mg	In stock	$ 786.00
100 mg	In stock	$ 1,090.00

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Purity: 99.90%

Biological Description

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Storage & Solubility Information

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

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)

References and Literature

1. Jung DW, et al. ACS Chem Biol. 2013, 8(6), 1271-1282.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Kinase Inhibitor Library Bioactive Compound Library Anti-Cancer Metabolism Compound Library Glycolysis Compound Library Anti-Cancer Compound Library NO PAINS Compound Library Metabolism Compound Library Glycometabolism Compound Library

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MK-0941 free base ML198 Dorzagliatin PF-04937319 AMG-1694 KAN0438757 Globalagliatin MitoPQ

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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.

Keywords

AP-III-a4 1177827-73-4 Metabolism Glucokinase Inhibitor AP-III-a-4 Phosphopyruvate hydratase Apoptosis inhibit antidiabetic anticancer HCT116 Enolase Huh7 zebrafish APIIIa4 ENOblock HEK AP III a4 inhibitor

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