1. Stem Cell/Wnt Metabolic Enzyme/Protease NF-κB Neuronal Signaling Membrane Transporter/Ion Channel Immunology/Inflammation
  2. Wnt Glutathione S-transferase NF-κB Calcium Channel NO Synthase
  3. Ethacrynic acid

Ethacrynic acid  (Synonyms: Etacrynic acid)

Art. -Nr.: HY-B1640 Reinheit: 99.90%
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Ethacrynic acid has anti-inflammatory and anticancer activity. Ethacrynic acid is an orally active diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferase (GSTs) and Wnt signaling pathways. Ethacrynic acid is a radiosensitizer. Ethacrynic acid can inhibit airway smooth muscle (ASM) contraction in mice. Ethacrynic acid can increase the outflow of aqueous humor from the eye for the study of glaucoma.

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CAS. Nr. : 58-54-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 9 publication(s) in Google Scholar

Other Forms of Ethacrynic acid:

Top Publications Citing Use of Products

    Ethacrynic acid purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Mar 31.  [Abstract]

    Mito-ros levels measured with MitoSOX red using a flow cytometer of SH-SY5Y cells pretreated with 10 μM AC220 for 2 h followed by cotreatment with or without 75 μM Ethacrynic acid (EA) for 24 h. n = 5; mean ± S.D.

    Ethacrynic acid purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Mar 31.  [Abstract]

    Representative microscopy images of SH-SY5Y cells pretreated with 10 μM AC220 for 2 h followed by cotreatment with or without 75 μM Ethacrynic acid (EA) for 24 h. Scale bar: 50 μm.

    Ethacrynic acid purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Mar 31.  [Abstract]

    PI positive of SH-SY5Y cells pretreated with 10 μM AC220 for 2 h followed by cotreatment with or without 75 μM Ethacrynic acid (EA) for 24 h. Scale bar: 50 μm.

    Ethacrynic acid purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Mar 31.  [Abstract]

    LDH release assay of SH-SY5Y cells pretreated with 10 μM AC220 for 2 h followed by cotreatment with or without 75 μM Ethacrynic acid (EA) for 24 h. Scale bar: 50 μm.

    Ethacrynic acid purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Mar 31.  [Abstract]

    Immunoblotting analysis for GSDME cleavage and activation of SH-SY5Y cell lysates pretreated with 10 μM AC220 for 2 h followed by cotreatment with or without 75 μM Ethacrynic acid (EA) treatment for 24 h. TUBB was used as loading control.

    Ethacrynic acid purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Mar 31.  [Abstract]

    Images of mice administered with AC220 (1.5 mg/kg), Ethacrynic acid (EA, 5 mg/kg, i.p. once daily) or AC220 (1.5 mg/kg) plus EA (5 mg/kg) every day.

    Ethacrynic acid purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Mar 31.  [Abstract]

    Ethacrynic acid (EA, 5 mg/kg, i.p. once daily). luciferase signal intensities of tumors were quantified using bioluminescence imaging.

    Ethacrynic acid purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Mar 31.  [Abstract]

    Ethacrynic acid (EA, 5 mg/kg, i.p. once daily). Images of SH-SY5Y orthotopic tumors. Scale bar: 1 cm.

    Alle Wnt Isoform-spezifische Produkte anzeigen:

    Alle NF-κB Isoform-spezifische Produkte anzeigen:

    Alle Calcium Channel Isoform-spezifische Produkte anzeigen:

    Alle NO Synthase Isoform-spezifische Produkte anzeigen:

    • Biologische Aktivität

    • Reinheit & Dokumentation

    • Verweise

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    Beschreibung

    Ethacrynic acid has anti-inflammatory and anticancer activity. Ethacrynic acid is an orally active diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferase (GSTs) and Wnt signaling pathways. Ethacrynic acid is a radiosensitizer. Ethacrynic acid can inhibit airway smooth muscle (ASM) contraction in mice. Ethacrynic acid can increase the outflow of aqueous humor from the eye for the study of glaucoma[1][2][3][4][5][6][7][8][9].

    IC50 & Target

    L-type calcium channel

     

    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    84 μM
    Compound: 1, EA
    Cytotoxicity against human A549 cells
    Cytotoxicity against human A549 cells
    [PMID: 22607679]
    CHO-K1 EC50
    56 μM
    Compound: 1
    Cytotoxicity against CHO-K1 cells by Alamar blue assay
    Cytotoxicity against CHO-K1 cells by Alamar blue assay
    [PMID: 16962325]
    HCT-116 IC50
    30.22 μM
    Compound: EA
    Cytotoxic activity against human HCT116 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Cytotoxic activity against human HCT116 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    [PMID: 27156773]
    HCT-116 IC50
    75 μM
    Compound: 1; EA
    Antiproliferative activity against human HCT116 cells after 24 to 72 hrs by MTS assay
    Antiproliferative activity against human HCT116 cells after 24 to 72 hrs by MTS assay
    [PMID: 27448922]
    HL-60 GI50
    44.2 μM
    Compound: EA
    Antiproliferative activity against human HL60 cells after 72 hrs
    Antiproliferative activity against human HL60 cells after 72 hrs
    [PMID: 17287120]
    HL-60 GI50
    44.2 μM
    Compound: EA
    Growth inhibition of human HL60 cells after 72 hrs by trypan blue staining
    Growth inhibition of human HL60 cells after 72 hrs by trypan blue staining
    [PMID: 22370342]
    HL-60 GI50
    45 μM
    Compound: EA
    Growth inhibition of human HL60 cells by hemocytometry
    Growth inhibition of human HL60 cells by hemocytometry
    [PMID: 20055416]
    HL-60 IC50
    3.4 μM
    Compound: EA
    Inhibition of GST P1-1 in human HL60 cell lysate
    Inhibition of GST P1-1 in human HL60 cell lysate
    [PMID: 20055416]
    HL-60 IC50
    38 μM
    Compound: 1; EA
    Cytotoxicity against human HL60 cells assessed as reduction in cell viability after 24 hrs by MTS assay
    Cytotoxicity against human HL60 cells assessed as reduction in cell viability after 24 hrs by MTS assay
    [PMID: 27448922]
    HL-60 IC50
    46 μM
    Compound: 1; EA
    Antiproliferative activity against human HL60 cells after 24 to 72 hrs by MTS assay
    Antiproliferative activity against human HL60 cells after 24 to 72 hrs by MTS assay
    [PMID: 27448922]
    HT-1080 IC50
    54.53 μM
    Compound: EA
    Cytotoxic activity against human HT1080 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Cytotoxic activity against human HT1080 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    [PMID: 27156773]
    HT-29 IC50
    62.39 μM
    Compound: EA
    Cytotoxic activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Cytotoxic activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    [PMID: 27156773]
    KB IC50
    11 μM
    Compound: 1; EA
    Antiproliferative activity against human KB cells after 24 to 72 hrs by MTS assay
    Antiproliferative activity against human KB cells after 24 to 72 hrs by MTS assay
    [PMID: 27448922]
    MCF7 IC50
    28.92 μM
    Compound: EA
    Cytotoxic activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Cytotoxic activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    [PMID: 27156773]
    MCF7 IC50
    41 μM
    Compound: 1; EA
    Antiproliferative activity against human MCF7 cells after 24 to 72 hrs by MTS assay
    Antiproliferative activity against human MCF7 cells after 24 to 72 hrs by MTS assay
    [PMID: 27448922]
    MDA-MB-231 IC50
    45.24 μM
    Compound: EA
    Cytotoxic activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Cytotoxic activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    [PMID: 27156773]
    MDA-MB-468 IC50
    81.45 μM
    Compound: EA
    Cytotoxic activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Cytotoxic activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    [PMID: 27156773]
    NCI-H1299 IC50
    44.29 μM
    Compound: EA
    Cytotoxic activity against human H1299 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Cytotoxic activity against human H1299 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    [PMID: 27156773]
    OVCAR-8 IC50
    72 μM
    Compound: 1; EA
    Antiproliferative activity against human OVCAR8 cells after 24 to 72 hrs by MTS assay
    Antiproliferative activity against human OVCAR8 cells after 24 to 72 hrs by MTS assay
    [PMID: 27448922]
    PC-3 IC50
    75 μM
    Compound: 1; EA
    Antiproliferative activity against human PC3 cells after 24 to 72 hrs by MTS assay
    Antiproliferative activity against human PC3 cells after 24 to 72 hrs by MTS assay
    [PMID: 27448922]
    SF-188 IC50
    31.65 μM
    Compound: EA
    Cytotoxic activity against human SF188 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Cytotoxic activity against human SF188 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    [PMID: 27156773]
    SK-BR-3 IC50
    34.21 μM
    Compound: EA
    Cytotoxic activity against human SKBR3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Cytotoxic activity against human SKBR3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    [PMID: 27156773]
    SK-OV-3 IC50
    > 100 μM
    Compound: 1; EA
    Antiproliferative activity against human SKOV3 cells after 24 to 72 hrs by MTS assay
    Antiproliferative activity against human SKOV3 cells after 24 to 72 hrs by MTS assay
    [PMID: 27448922]
    SW480 IC50
    32.7 μM
    Compound: 1
    Inhibition of Wnt/beta-casein signaling in human SW480 cells by fluorimetry
    Inhibition of Wnt/beta-casein signaling in human SW480 cells by fluorimetry
    [PMID: 19121941]
    In Vitro

    Ethacrynic acid (50 μM; 24 h) inhibits Wnt/β-catenin signaling in CLL cells[1].
    Ethacrynic acid (1-100 μM; 48 h) is cytotoxic in CLL cells with an IC50 of 8.56 μM[1].
    Ethacrynic acid (0.01-0.25 mmol/L; 30 min) increases aqueous humor outflow facility acutely in eye and the outflow rate increases from 28% to 105%[2].
    Ethacrynic acid (10-100 μM; 30 min) can inhibit the activation of NF-κB pathway in RAW264.7 cells induced by LPS (100 ng/mL) and has anti-inflammatory activity[3].
    Ethacrynic acid (20 μM/mL; 2 h) can increase the radiation intensity in MCF-7 cancer cells after radiation exposure[3].
    Ethacrynic acid (100 μmol/L; 62.5-250 min) inhibits tracheal ring contraction induced by high -K+ (80 mmol/L) and acetylcholine (ACh, 100 µmol/L) in a dose-dependent manner with EC50 of 40.28 µmol/L and 56.22 µmol/L, respectively[8].
    Ethacrynic acid (100 μmol/L; 500-2500 s) decreases the intracellular Ca2+ concentration induced by high -K+ and ACh from 0.40 to 0.16, 0.50 to 0.39, respectively[8].

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

    RT-PCR[1]

    Cell Line: Chronic lymphocytic leukemia (CLL)
    Concentration: 1 μM, 10 μM, 100 μM
    Incubation Time: 16 h
    Result: Depressed the expression of LEF-1, Cyclin D1 and Fibronectin in a concentration-dependent manner.( LEF-1, cyclin D1 and fibronectin are established target genes of the Wnt/b-catenin pathway).

    Western Blot Analysis[3]

    Cell Line: RAW 264.7
    Concentration: 10 μM, 20 μM, 50 μM, 100 μM ;Before LPS treatment (100 ng/mL; 1 h)
    Incubation Time: 30 min
    Result: Inhibited the expression of iNOS mRNA.
    Inhibited degradation of IκBα and IκBβ.
    In Vivo

    Ethacrynic acid (450 μg/mouse; Oral gavage; Once daily for 60 days) can inhibit tumor growth in the mice[5].

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

    Animal Model: Myeloma Balb/c mice model[5]
    Dosage: 450 μg/mouse
    Administration: Oral gavage (p.o.); Once daily for 60 days. After BALB/c mice were injected subcutaneously with 5 × 105 MPC11 myeloma cells.
    Result: Significantly inhibited tumor growth.
    Klinische Studie
    Molekulargewicht

    303.14

    Formel

    C13H12Cl2O4

    CAS. Nr.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(O)COC1=CC=C(C(C(CC)=C)=O)C(Cl)=C1Cl

    Versand

    Room temperature in continental US; may vary elsewhere.

    Speicherung

    4°C, protect from light

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

    Lösungsmittel & Löslichkeit
    In Vitro: 

    DMSO : 100 mg/mL (329.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 27.5 mg/mL (90.72 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.2988 mL 16.4940 mL 32.9881 mL
    5 mM 0.6598 mL 3.2988 mL 6.5976 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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    * 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.

    • Molaritätsrechner

    • Verdünnungsrechner

    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 (8.25 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 (8.25 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  PBS

      Solubility: 1 mg/mL (3.30 mM); Clear solution; Need ultrasonic

    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.
    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).
    Reinheit & Dokumentation

    Purity: 99.98%

    Verweise

    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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 3.2988 mL 16.4940 mL 32.9881 mL 82.4701 mL
    5 mM 0.6598 mL 3.2988 mL 6.5976 mL 16.4940 mL
    10 mM 0.3299 mL 1.6494 mL 3.2988 mL 8.2470 mL
    15 mM 0.2199 mL 1.0996 mL 2.1992 mL 5.4980 mL
    20 mM 0.1649 mL 0.8247 mL 1.6494 mL 4.1235 mL
    25 mM 0.1320 mL 0.6598 mL 1.3195 mL 3.2988 mL
    30 mM 0.1100 mL 0.5498 mL 1.0996 mL 2.7490 mL
    40 mM 0.0825 mL 0.4124 mL 0.8247 mL 2.0618 mL
    50 mM 0.0660 mL 0.3299 mL 0.6598 mL 1.6494 mL
    60 mM 0.0550 mL 0.2749 mL 0.5498 mL 1.3745 mL
    80 mM 0.0412 mL 0.2062 mL 0.4124 mL 1.0309 mL
    DMSO 100 mM 0.0330 mL 0.1649 mL 0.3299 mL 0.8247 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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    Produktname:
    Ethacrynic acid
    Art. -Nr.:
    HY-B1640
    Menge:
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