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

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.

For research use only. We do not sell to patients.

AP-III-a4 Chemical Structure

AP-III-a4 Chemical Structure

CAS No. : 1177827-73-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 196 In-stock
Solution
10 mM * 1 mL in DMSO USD 196 In-stock
Solid
1 mg USD 60 In-stock
5 mg USD 150 In-stock
10 mg USD 250 In-stock
25 mg USD 470 In-stock
50 mg USD 750 In-stock
100 mg USD 1250 In-stock
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of AP-III-a4:

AP-III-a4 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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]
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.

AP-III-a4 Related Antibodies

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.
Molecular Weight

594.72

Formula

C31H43FN8O3
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

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

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6815 mL 8.4073 mL 16.8146 mL
5 mM 0.3363 mL 1.6815 mL 3.3629 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, 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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: ≥ 2.5 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.

    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: 2.5 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.

    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, 6 months; -20°C, 1 month (protect from light)

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.
Purity & Documentation

Purity: 99.87%

COA (244 KB) HNMR (384 KB) RP-HPLC (266 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
References

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, 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.

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
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AP-III-a4 Related Classifications

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-a41177827-73-4ENOblockEnolaseApoptosisPhosphopyruvate hydrataseanticancerHCT116zebrafishHuh7HEKantidiabeticInhibitorinhibitorinhibit

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