2. Stem Cell/Wnt NF-κB GPCR/G Protein PI3K/Akt/mTOR Metabolic Enzyme/Protease TGF-beta/Smad Apoptosis Neuronal Signaling
  3. Akt Adrenergic Receptor mTOR NF-κB Dopamine β-hydroxylase TGF-beta/Smad Apoptosis PI3K
  4. Fusaric acid

Fusaric acid is an orally active multi-pathway inhibitor with the activity of inducing oxidative stress and apoptosis. Fusaric acid can chelate divalent metal cations, damage mitochondrial membrane structure, and activate apoptosis-related proteases such as Caspase-3/7, -8, and -9. Fusaric acid also regulates Bax/Bcl-2 protein, inhibits fibrosis-related signaling pathways such as NF-κB, TGF-β1/SMADs, and PI3K/AKT/mTOR, and reduces collagen deposition. Fusaric acid is also a dopamine β-hydroxylase inhibitor, which reduces endogenous levels of norepinephrine and epinephrine in the brain, heart, spleen, and adrenal glands. Fusaric acid can play a role in myocardial fibrosis and improve cardiac hypertrophy in heart disease, and can also be used in the study of esophageal cancer and liver cancer.

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Fusaric acid Chemical Structure

Fusaric acid Chemical Structure

CAS No. : 536-69-6

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Based on 1 publication(s) in Google Scholar

Other Forms of Fusaric acid:

Fusaric acid Related Antibodies

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Description

Fusaric acid is an orally active multi-pathway inhibitor with the activity of inducing oxidative stress and apoptosis. Fusaric acid can chelate divalent metal cations, damage mitochondrial membrane structure, and activate apoptosis-related proteases such as Caspase-3/7, -8, and -9. Fusaric acid also regulates Bax/Bcl-2 protein, inhibits fibrosis-related signaling pathways such as NF-κB, TGF-β1/SMADs, and PI3K/AKT/mTOR, and reduces collagen deposition. Fusaric acid is also a dopamine β-hydroxylase inhibitor, which reduces endogenous levels of norepinephrine and epinephrine in the brain, heart, spleen, and adrenal glands. Fusaric acid can play a role in myocardial fibrosis and improve cardiac hypertrophy in heart disease, and can also be used in the study of esophageal cancer and liver cancer[1][2][3][4].

In Vitro

Fusaric acid (0-500 μg/mL; 24 h) inhibits cell viability in a dose-dependent manner in human esophageal cancer cells (SNO) with an IC50 value of 78.81 μg/mL[1].
Fusaric acid (100 μM; 24-72 h) induces programmed cell death in tobacco suspension cells, accompanied by H2O2 accumulation, decreases mitochondrial membrane potential, and activation of caspase-3-like proteases[2].
Fusaric acid (0-160 μM; 24-96 h) inhibits the cell viability of rat cardiomyocytes (H9C2) and mouse cardiac fibroblasts (mCFs), and suppresses the expression of fibrosis-related proteins (α-SMA, type I/III collagen) in WB results at 24 h, and downregulates TGF-β1/SMADs and PI3K/AKT signaling pathways[3].

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

Fusaric acid Related Antibodies

Cell Viability Assay[1]

Cell Line: Cardiomyocytes isolated from mice, Rat cardiomyocytes (H9C2) and Mouse cardiac fibroblasts (mCFs)
Concentration: 1.25 μM, 2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM, 80 μM, 160 μM
Incubation Time: 6 h, 12 h, 24 h, 36 h, 48 h, 72 h, 96 h
Result: Only at the high concentration of 80 and 160 uM for long time (72 and 96 h), significant difference in cells, indicating a relatively low doses for time under 96 h showed no obvious cytotoxicity to cardiomyocytes isolated from mice and H9C2 cells.
In Vivo

Fusaric acid (50, 100 mg/kg; gavage; once a day; pretreatment for 7 days + continuous for 7 days) reduces myocardial fibrosis in the Isoprenaline (HY-B0468)-induced cardiac hypertrophy model in mice, reduces the heart weight/body weight ratio and heart weight/tibia length ratio, improves left ventricular function, and inhibits TGF-β1/SMADs and PI3K/AKT signaling pathways[3].

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

Animal Model: Male C57BL/6 mice (18-22 g, 8 weeks old) with Isoprenaline (HY-B0468)-induced cardiac hypertrophy and fibrosis[3]
Dosage: 50 mg/kg, 100 mg/kg
Administration: Oral gavage daily for 7 days before Isoprenaline treatment, then continued for another 7 days (total 15 days)
Result: Cardiac hypertrophy markers:
Reduced heart weight/body weight and heart weight/tibia length ratios compared to the Isoprenaline group, indicating attenuated cardiac hypertrophy.
Histological analysis:
Masson's trichrome staining showed decreased collagen deposition in heart tissues, with reduced fibrosis area compared to the Isoprenaline group. WGA staining revealed smaller cardiomyocyte cross-sectional area, indicating attenuated myocyte hypertrophy.
Echocardiography:
Improved left ventricular function, including increased fractional shortening (FS%) and reduced left ventricular end-diastolic/systolic dimensions, compared to the Isoprenaline group.
Molecular Weight

179.22

Formula

C10H13NO2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=NC=C(CCCC)C=C1)O
Structure Classification
Initial Source

Fusarium spp.
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (348.73 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 50 mg/mL (278.99 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.5797 mL 27.8987 mL 55.7973 mL
5 mM 1.1159 mL 5.5797 mL 11.1595 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.

* 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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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: ≥ 2.08 mg/mL (11.61 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 (11.61 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

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g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.94%

SDS (392 KB)

COA (243 KB) HNMR (252 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. 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
H2O / DMSO 1 mM 5.5797 mL 27.8987 mL 55.7973 mL 139.4934 mL
5 mM 1.1159 mL 5.5797 mL 11.1595 mL 27.8987 mL
10 mM 0.5580 mL 2.7899 mL 5.5797 mL 13.9493 mL
15 mM 0.3720 mL 1.8599 mL 3.7198 mL 9.2996 mL
20 mM 0.2790 mL 1.3949 mL 2.7899 mL 6.9747 mL
25 mM 0.2232 mL 1.1159 mL 2.2319 mL 5.5797 mL
30 mM 0.1860 mL 0.9300 mL 1.8599 mL 4.6498 mL
40 mM 0.1395 mL 0.6975 mL 1.3949 mL 3.4873 mL
50 mM 0.1116 mL 0.5580 mL 1.1159 mL 2.7899 mL
60 mM 0.0930 mL 0.4650 mL 0.9300 mL 2.3249 mL
80 mM 0.0697 mL 0.3487 mL 0.6975 mL 1.7437 mL
100 mM 0.0558 mL 0.2790 mL 0.5580 mL 1.3949 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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Fusaric acid Related Classifications

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    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:

Fusaric acid536-69-6AktAdrenergic ReceptormTORNF-κBDopamine β-hydroxylaseTGF-beta/SmadApoptosisPI3KPKBProtein kinase BBeta ReceptorMammalian target of RapamycinNuclear factor-κBNuclear factor-kappaBDopamine beta-hydroxylaseDopamine beta-monooxygenaseDopamine β-monooxygenaseTransforming growth factor betaPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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