| Field | Specification |
|---|---|
| Alternative names | ENOblock |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C31H43FN8O3 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
AP-III-a4, also known as ENOblock, is a nonsubstrate analogue inhibitor of enolase with an IC50 of 0.576 μM. It can be used in the research of cancer and diabetes[1]. It is supplied as an off-white to light yellow solid (C31H43FN8O3, MW 594.72) at 99.37% purity.
Physical & Chemical Properties
| CAS Number | 1177827-73-4 |
|---|---|
| Molecular Formula | C31H43FN8O3 |
| Molecular Weight | 594.72 g/mol |
| Purity | 99.37% |
| Appearance | Solid |
| 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 |
| Signaling Pathway | Metabolic Enzyme/Protease; Apoptosis |
| Solubility | In Vitro: DMSO: 100 mg/mL (168.15 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) H2O: < 0.1 mg/mL (insoluble) |
| Storage | 4°C, protect from light. In solvent: -80°C, 6 months; -20°C, 1 month (protect from light). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
IC50: 0.576 μM (enolase)[1]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (168.15 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
| H2O | < 0.1 mg/mL | insoluble |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); protect from light; avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (4.20 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | 2.5 mg/mL (4.20 mM); suspension; requires sonication |
| How to prepare | Gives a suspension at 2.5 mg/mL. The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (4.20 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
AP-III-a4 (ENOblock) (0-10 μM; 24 h) reduces HCT116 cell viability in a dose-dependent manner[1]. AP-III-a4 binds enolase directly and inhibits its activity[1]. At 0-10 μM (24 or 48 h), AP-III-a4 inhibits cancer cell migration and invasion and induces cancer cell apoptosis[1]. In hepatocytes and kidney cells, AP-III-a4 (10 μM; 24 h) can induce glucose uptake and inhibit expression of phosphoenolpyruvate carboxykinase (PEPCK)[1].
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
In zebrafish, AP-III-a4 (ENOblock) at 10 μM for 96 h inhibits cancer cell metastasis and suppresses PEPCK, a regulator of gluconeogenesis[1].
| 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Integrative plasma and fecal metabolomics identify functional metabolites in adenoma-colorectal cancer progression and as early diagnostic biomarkers. Cancer Cell 2024 Aug 12;42(8):1386-1400.e8. PMID: 39137727
Oncogenic Fatty Acid Metabolism Rewires Energy Supply Chain in Gastric Carcinogenesis. Gastroenterology 2024 May;166(5):772-786.e14. PMID: 38272100
The glycolytic metabolite phosphoenolpyruvate restricts cGAS-driven inflammation to promote healthy aging. Nat Aging 2026 Apr;6(4):831-848. PMID: 41792330
Single-Cell Lineage Tracing Uncovers Resistance Signatures and Sensitizing Strategies to FLT3 Inhibitors in Acute Myeloid Leukemia. Cancer Res 2025 Nov 21:10.1158/0008-5472.CAN-24-3753. PMID: 41270153
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. Nat Commun 2026 Feb 12;17(1):1214. PMID: 41680175
A bioenergetic shift is required for spermatogonial differentiation. Cell Discov 2020 Aug 18:6:56. PMID: 32864161
Inhibition of HSP90β Improves Lipid Disorders by Promoting Mature SREBPs Degradation via the Ubiquitin-proteasome System. Theranostics 2019 Aug 12;9(20):5769-5783.
Acta Pharm Sin B. 2026 Mar 14.
Proviral insights of glycolytic enolase in Bamboo mosaic virus replication associated with chloroplasts and mitochondria. Proc Natl Acad Sci U S A 2025 May 13;122(19):e2415089122. PMID: 40327700
ENOblock synergizes with colistin to treat Acinetobacter baumannii infections. EMBO Mol Med 2025 Dec;17(12):3496-3524. PMID: 41174184
