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

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

Cat. No.: HY-15858A Purity: 99.24%
SDS COA Handling Instructions

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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.

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

AP-III-a4 hydrochloride Chemical Structure

AP-III-a4 hydrochloride Chemical Structure

CAS No. : 2070014-95-6

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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of AP-III-a4 hydrochloride:

AP-III-a4 hydrochloride Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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]
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 hydrochloride 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

631.18

Formula

C31H44ClFN8O3
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

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
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
=
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: ≥ 2.08 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.
Purity & Documentation

Purity: 99.24%

SDS (252 KB)

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

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  • 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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