2. Cell Cycle/DNA Damage Epigenetics
  3. Sirtuin
  4. 2-APQC

2-APQC is an orally active and selective agonist of Sirtuin-3 (SIRT3) (Kd=2.756 μM), antagonizes Isoproterenol/ISO (HY-B0468)-induced cytotoxicity. 2-APQC activates the SIRT3-PYCR1 axis to enhance mitochondrial proline metabolism and inhibit the ROS-p38MAPK pathway by inhibiting signaling pathways such as mTOR-p70S6K, JNK, and TGF-β/Smad3. 2-APQC also activates the AMPK-Parkin axis to alleviate myocardial hypertrophy and fibrosis and protect cardiac function. 2-APQC can be used in the study of heart failure.

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2-APQC Chemical Structure

2-APQC Chemical Structure

CAS No. : 500271-63-6

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Based on 1 publication(s) in Google Scholar

2-APQC Related Antibodies

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Description

2-APQC is an orally active and selective agonist of Sirtuin-3 (SIRT3) (Kd=2.756 μM), antagonizes Isoproterenol/ISO (HY-B0468)-induced cytotoxicity. 2-APQC activates the SIRT3-PYCR1 axis to enhance mitochondrial proline metabolism and inhibit the ROS-p38MAPK pathway by inhibiting signaling pathways such as mTOR-p70S6K, JNK, and TGF-β/Smad3. 2-APQC also activates the AMPK-Parkin axis to alleviate myocardial hypertrophy and fibrosis and protect cardiac function. 2-APQC can be used in the study of heart failure[1].

IC50 & Target

SIRT3

2.756 (Kd)

In Vitro

2-APQC (1, 10, 100 μM; 24 h) activates SIRT3 deacetylation activity in H9c2 cells in a concentration-dependent manner[1].
2-APQC (40 μM; 24 h) has no significant cytotoxicity to H9c2 cells[1].
2-APQC (1-100 μM; 24 h pretreatment + ISO treatment for 48 h) improves Isoproterenol/ISO (HY-B0468)-induced decrease in H9c2 cell viability, attenuates ISO-induced cardiomyocyte hypertrophy at a dose of 10 μM, and reduces the expression of α-SMA and collagen I[1].
2-APQC (10 μM; 24 h) reduces AcK68-MnSOD2, AcK122-MnSOD2 and acetylated lysine levels in H9c2 cells, without significantly change SIRT3 protein expression[1].

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

2-APQC Related Antibodies

Cell Viability Assay[1]

Cell Line: H9c2 cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Decreased the levels of acetylated lysine, AcK68-MnSOD2, and AcK122-MnSOD2, indicating enhanced SIRT3 deacetylation activity.
Didn't change the expression of SIRT3 protein level.
In Vivo

2-APQC (10-30 mg/kg; oral gavage; once a day; 4 weeks) can improve cardiac ejection fraction (EF) and shortening fraction (FS), reduce left ventricular end-systolic diameter (LVESD) and brain natriuretic peptide (BNP) levels, reduce myocardial hypertrophy and fibrosis, and reduce serum levels of myocardial injury markers such as lactate dehydrogenase (LDH) and aspartate aminotransferase (AST) in the Isoproterenol/ISO (HY-B0468)-induced rat heart failure model[1].
2-APQC (42 mg/kg; intraperitoneal injection; once a day; 4 weeks) can improve cardiac function and reduce myocardial injury in the ISO-induced wild-type male mouse heart failure model, while this protective effect disappears in SIRT3 knockout mice[1].

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

Animal Model: Male SD rats (220-250 g), ISO-induced heart failure model[1]
Dosage: 10, 20, 30 mg/kg
Administration: Gavage, once daily, 4 weeks; while ISO groups were injected subcutaneously with 5 mg/kg/d for 2 weeks. After the model was successfully established, 3 mL/kg/d normal saline was fed to rats.
Result: Significantly improved cardiac function as evidenced by increased EF and FS, decreased LVESD and LVPWD, and reduced BNP levels.
Alleviated myocardial hypertrophy and fibrosis, as shown by decreased heart weight index, reduced collagen fiber deposition in Sirius Red staining, and smaller myocyte cross-sectional area in WGA staining.
Serum levels of LDH, AST, CK-MB, and α-HBDH were decreased, indicating reduced myocardial injury.
Molecular Weight

405.47

Formula

C23H24FN5O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CCCCCNC(C1=C(N(C2=NC3=C(N=C21)C=CC=C3)CC4=CC=C(C=C4)F)N)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (123.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4663 mL 12.3314 mL 24.6627 mL
5 mM 0.4933 mL 2.4663 mL 4.9325 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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 (6.17 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 (6.17 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 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:

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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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).
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: 99.70%

SDS (252 KB)

COA (256 KB) HNMR (260 KB) LCMS (93 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. 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 2.4663 mL 12.3314 mL 24.6627 mL 61.6568 mL
5 mM 0.4933 mL 2.4663 mL 4.9325 mL 12.3314 mL
10 mM 0.2466 mL 1.2331 mL 2.4663 mL 6.1657 mL
15 mM 0.1644 mL 0.8221 mL 1.6442 mL 4.1105 mL
20 mM 0.1233 mL 0.6166 mL 1.2331 mL 3.0828 mL
25 mM 0.0987 mL 0.4933 mL 0.9865 mL 2.4663 mL
30 mM 0.0822 mL 0.4110 mL 0.8221 mL 2.0552 mL
40 mM 0.0617 mL 0.3083 mL 0.6166 mL 1.5414 mL
50 mM 0.0493 mL 0.2466 mL 0.4933 mL 1.2331 mL
60 mM 0.0411 mL 0.2055 mL 0.4110 mL 1.0276 mL
80 mM 0.0308 mL 0.1541 mL 0.3083 mL 0.7707 mL
100 mM 0.0247 mL 0.1233 mL 0.2466 mL 0.6166 mL
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2-APQC 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:

2-APQC500271-63-6Sirtuincardiac fibrosismyocardial fibrosisheart failureISO-induced HF modelInhibitorinhibitorinhibit

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