Art. -Nr.: HY-15858

AP-III-a4

(Synonyms: ENOblock)

17 Cited Publications

Kundenbewertung

Based on 17 publication(s) in Google Scholar

AP-III-a4 (ENOblock) is a nonsubstrate analogue enolase inhibitor with an IC₅₀ of 0.576 uM. AP-III-a4 can be used for the research of cancer and diabetic.

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Reinheit: 99.87%
CAS. Nr.: 1177827-73-4
Formel: C₃₁H₄₃FN₈O₃
Molecular Weight:594.72

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

AP-III-a4 Chemical Structure

CAS. Nr.: 1177827-73-4

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (17)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

AP-III-a4 (ENOblock) is a nonsubstrate analogue enolase inhibitor with an IC₅₀ of 0.576 uM. AP-III-a4 can be used for the research of cancer and diabetic^[1].

IC₅₀ & Target

IC₅₀: 0.576 uM (enolase)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HUVEC	IC₅₀	48.25 μg/mL Compound: ENOblock	Cytotoxicity against human HUVEC cells assessed as cell viability measured after 24 hrs by CCK-8 assay Cytotoxicity against human HUVEC cells assessed as cell viability measured after 24 hrs by CCK-8 assay	[PMID: 38381075]

In Vitro

AP-III-a4 (ENOblock) (0-10 μM; 24 h) inhibits HCT116 cell viability in a dose-dependent manner^[1].
AP-III-a4 directly binds to enolase and inhibits its activity^[1].
AP-III-a4 (0-10 μM; 24 or 48 h) inhibits cancer cell migration and invasion, induces cancer cell apoptosis^[1].
AP-III-a4 (10 μM; 24 h) can induce glucose uptake and inhibit phosphoenolpyruvate carboxykinase (PEPCK) expression in hepatocytes and kidney cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

HCT116
Concentration:

1.25, 2.5, 5 and 10 μM
Incubation Time:

24 h
Result:

Induced higher levels of HCT116 colon cancer cell death in hypoxic conditions compared to normoxia.

Western Blot Analysis^[1]

Cell Line:

HCT116
Concentration:

1.25, 2.5, 5 and 10 μM
Incubation Time:

24 h for AKT, 48 h for Bcl-Xl
Result:

Bound to enolase in cell lysate and bound to purified enolase.
Decreased the expression of AKT and Bcl-Xl, which are negative regulators of apoptosis.

Cell Invasion Assay^[1]

Cell Line:

HCT116
Concentration:

0.156, 0.312, 0.625, 1.25 and 2.5 μM
Incubation Time:

24 h
Result:

Significantly inhibits cancer cell invasion at a treatment concentration of 0.625 μM.

Cell Migration Assay ^[1]

Cell Line:

HCT116
Concentration:

0.625, 1.25 and 2.5 μM
Incubation Time:

24 h
Result:

Inhibited cell migration dose-dependently.

RT-PCR^[1]

Cell Line:

Huh7 and HEK
Concentration:

10 μM
Incubation Time:

24 h
Result:

Induced glucose uptake and inhibited PEPCK expression.

In Vivo

AP-III-a4 (ENOblock) (10 μM; 96 h) inhibits cancer cell metastasis and suppresses the gluconeogenesis regulator PEPCK in zebrafish^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

The zebrafish cancer cell HCT116 xenograft model^[1]
Dosage:

10 μM
Administration:

96 h
Result:

Reduced cancer cell dissemination. Inhibited PEPCK expression and induced glucose uptake. Inhibited adipogenesis and foam cell formation.

Chemical Information

CAS. Nr. 1177827-73-4
Appearance Solid
Molecular Weight 594.72
Formel C₃₁H₄₃FN₈O₃
Color Off-white to light yellow
SMILES

FC1=CC=C(CNC2=NC(NCC3CCCCC3)=NC(NC4=CC=C(CC(NCCOCCOCCN)=O)C=C4)=N2)C=C1
Synonyms

ENOblock
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (17)

All Bio/Physico-chemical AssayCell Proliferation/Viability AssayRT-PCRWB

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Journal Impact Factor

Cancer Cell

Integrative plasma and fecal metabolomics identify functional metabolites in adenoma-colorectal cancer progression and as early diagnostic biomarkers. [Abstract]

2024 Aug 12;42(8):1386-1400.e8. PMID: 39137727

AP-III-a4 purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2024 Aug 12;42(8):1386-1400.e8. [Abstract]

ENO1 antagonist AP-III-a4 (10 μM) reversed the increase in viability of CRC cells (HCT116, HT-29) induced by oleic acid.

AP-III-a4 purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2024 Aug 12;42(8):1386-1400.e8. [Abstract]

ENO1 antagonist AP-III-a4 (10 μM) reversed the increased protein expression of phosphorylated JAK1, PI3K, and AKT in human CRC cells (HCT116, HT-29) induced by oleic acid.
Gastroenterology

Oncogenic Fatty Acid Metabolism Rewires Energy Supply Chain in Gastric Carcinogenesis. [Abstract]

2024 Jan 24:S0016-5085(24)00064-7. PMID: 38272100
Nat Aging

The glycolytic metabolite phosphoenolpyruvate restricts cGAS-driven inflammation to promote healthy aging. [Abstract]

2026 Apr;6(4):831-848. PMID: 41792330
Cancer Res

Single-Cell Lineage Tracing Uncovers Resistance Signatures and Sensitizing Strategies to FLT3 Inhibitors in Acute Myeloid Leukemia. [Abstract]

2025 Nov 21:10.1158/0008-5472.CAN-24-3753. PMID: 41270153
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Cell Discov

A bioenergetic shift is required for spermatogonial differentiation. [Abstract]

2020 Aug 18;6:56. PMID: 32864161
Theranostics

Inhibition of HSP90β Improves Lipid Disorders by Promoting Mature SREBPs Degradation via the Ubiquitin-proteasome System. [Abstract]

2019 Aug 12;9(20):5769-5783. PMID: 31534518

AP-III-a4 purchased from MedChemExpress. Usage Cited in: Theranostics. 2019 Aug 12;9(20):5769-5783. [Abstract]

ENO1 concentration was kept constant at 20 nM and the small molecule was titrated from AP-III-a4 (50 μM).
Acta Pharm Sin B

2026 Mar 14.
Proc Natl Acad Sci U S A

Proviral insights of glycolytic enolase in Bamboo mosaic virus replication associated with chloroplasts and mitochondria. [Abstract]

2025 May 13;122(19):e2415089122. PMID: 40327700

AP-III-a4 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2025 May 13;122(19):e2415089122. [Abstract]

AP-III-a4 (ENOblock) (20 μM; 16 h) significantly reduced the size of BaMV VRC clusters of 3-wk-old WT N. benthamiana.

AP-III-a4 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2025 May 13;122(19):e2415089122. [Abstract]

AP-III-a4 (ENOblock) (20 μM; 16 h) significantly reduced the BaMV titer of 3-wk-old WT N. benthamiana.
EMBO Mol Med

ENOblock synergizes with colistin to treat Acinetobacter baumannii infections. [Abstract]

2025 Dec;17(12):3496-3524. PMID: 41174184
Int J Mol Sci

Paeoniflorin Directly Targets ENO1 to Inhibit M1 Polarization of Microglia/Macrophages and Ameliorates EAE Disease. [Abstract]

2025 Apr 13;26(8):3677. PMID: 40332313
Cancers (Basel)

Cinnamaldehyde Enhances Antimelanoma Activity through Covalently Binding ENO1 and Exhibits a Promoting Effect with Dacarbazine. [Abstract]

2020 Jan 29;12(2):311. PMID: 32013122
Biomedicines

HIF-1α Promotes Macrophage Extracellular Trap Formation and Exacerbates Acute Lung Injury in Neonatal Sepsis. [Abstract]

2026 May 18;14(5):1145. PMID: 42193470
bioRxiv

2024 October 25.
Biomed Pharmacother

Ciwujianoside E inhibits Burkitt lymphoma cell proliferation and invasion by blocking ENO1-plasminogen interaction and TGF-β1 activation. [Abstract]

2024 Jun 18:177:116970. PMID: 38897160
SSRN

2023 Feb 10.
Research Square Print

November 14th, 2022

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (168.15 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6815 mL

8.4073 mL

16.8146 mL

5 mM

0.3363 mL

1.6815 mL

3.3629 mL

10 mM

0.1681 mL

0.8407 mL

1.6815 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.20 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (4.20 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.20 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Da-Woon Jung, et al. A Unique Small Molecule Inhibitor of Enolase Clarifies Its Role in Fundamental Biological Processes.ACS Chem. Biol., 2013, 8 (6), pp 1271–1282 [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.6815 mL	8.4073 mL	16.8146 mL	42.0366 mL
	5 mM	0.3363 mL	1.6815 mL	3.3629 mL	8.4073 mL
	10 mM	0.1681 mL	0.8407 mL	1.6815 mL	4.2037 mL
	15 mM	0.1121 mL	0.5605 mL	1.1210 mL	2.8024 mL
	20 mM	0.0841 mL	0.4204 mL	0.8407 mL	2.1018 mL
	25 mM	0.0673 mL	0.3363 mL	0.6726 mL	1.6815 mL
	30 mM	0.0560 mL	0.2802 mL	0.5605 mL	1.4012 mL
	40 mM	0.0420 mL	0.2102 mL	0.4204 mL	1.0509 mL
	50 mM	0.0336 mL	0.1681 mL	0.3363 mL	0.8407 mL
	60 mM	0.0280 mL	0.1401 mL	0.2802 mL	0.7006 mL
	80 mM	0.0210 mL	0.1051 mL	0.2102 mL	0.5255 mL
	100 mM	0.0168 mL	0.0841 mL	0.1681 mL	0.4204 mL

Keywords

AP-III-a4

17 Cited Publications

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AP-III-a4

Apoptosis Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-diabetic Compound Library

Glycolysis Compound Library

Anti-Cancer Metabolism Compound Library

Glucose Metabolism Compound Library

Metabolic Enzyme Compound Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) AP-III-a4

Biologische Aktivität

Chemical Information

Publications (17)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AP-III-a4

Apoptosis Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-diabetic Compound Library

Glycolysis Compound Library

Anti-Cancer Metabolism Compound Library

Glucose Metabolism Compound Library

Metabolic Enzyme Compound Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) AP-III-a4

Biologische Aktivität

Chemical Information

Publications (17)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AP-III-a4 Related Classifications

HY-15858 Related Classifications