2. Metabolic Enzyme/Protease Apoptosis
  3. Enolase Apoptosis
  4. AP-III-a4 hydrochloride

AP-III-a4 hydrochloride  (Synonyms: ENOblock hydrochloride)

製品番号: HY-15858A 純度: 99.24%
COA 取扱説明書 Technical Support

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

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CAS 番号 : 2070014-95-6

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 208 在庫あり
Solution
10 mM * 1 mL in DMSO USD 208 在庫あり
Solid
5 mg $150 在庫あり
10 mg $250 在庫あり
25 mg $470 在庫あり
50 mg $750 在庫あり
100 mg $1250 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 16 publication(s) in Google Scholar

Other Forms of AP-III-a4 hydrochloride:

AP-III-a4 hydrochloride 関連抗体

Top Publications Citing Use of Products

    AP-III-a4 hydrochloride 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 hydrochloride 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.

    AP-III-a4 hydrochloride 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 hydrochloride 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.

    AP-III-a4 hydrochloride 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).

    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

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

    IC50 & Target

    IC50: 0.576 uM (enolase)[1]
    体外実験

    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.

    AP-III-a4 hydrochloride 関連抗体

    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.
    体内実験

    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.
    分子量

    631.18

    分子式

    C31H44ClFN8O3
    CAS 番号
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    FC1=CC=C(CNC2=NC(NCC3CCCCC3)=NC(NC4=CC=C(CC(NCCOCCOCCN)=O)C=C4)=N2)C=C1.Cl
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 53 mg/mL (83.97 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 12.5 mg/mL (19.80 mM; Need ultrasonic)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5843 mL 7.9217 mL 15.8433 mL
    5 mM 0.3169 mL 1.5843 mL 3.1687 mL
    10 mM 0.1584 mL 0.7922 mL 1.5843 mL
    View the Complete Stock Solution Preparation Table

    * 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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

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    体積 （終了）

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    体内:

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

    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: ≥ 2.08 mg/mL (3.30 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

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

      Solubility: ≥ 2.08 mg/mL (3.30 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.24%

    COA (245 KB) HNMR (289 KB) LCMS (96 KB)

    取扱説明書 (2659 KB)
    参考文献

    Complete Stock Solution Preparation Table

    * 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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 1.5843 mL 7.9217 mL 15.8433 mL 39.6084 mL
    5 mM 0.3169 mL 1.5843 mL 3.1687 mL 7.9217 mL
    10 mM 0.1584 mL 0.7922 mL 1.5843 mL 3.9608 mL
    15 mM 0.1056 mL 0.5281 mL 1.0562 mL 2.6406 mL
    DMSO 20 mM 0.0792 mL 0.3961 mL 0.7922 mL 1.9804 mL
    25 mM 0.0634 mL 0.3169 mL 0.6337 mL 1.5843 mL
    30 mM 0.0528 mL 0.2641 mL 0.5281 mL 1.3203 mL
    40 mM 0.0396 mL 0.1980 mL 0.3961 mL 0.9902 mL
    50 mM 0.0317 mL 0.1584 mL 0.3169 mL 0.7922 mL
    60 mM 0.0264 mL 0.1320 mL 0.2641 mL 0.6601 mL
    80 mM 0.0198 mL 0.0990 mL 0.1980 mL 0.4951 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    AP-III-a4 hydrochloride Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    質量   濃度   体積   分子量 *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    AP-III-a42070014-95-6ENOblockEnolaseApoptosisPhosphopyruvate hydrataseanticancerHCT116zebrafishHuh7HEKantidiabeticInhibitorinhibitorinhibit

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    製品名:
    AP-III-a4 hydrochloride
    製品番号:
    HY-15858A
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