1. Neuronal Signaling Membrane Transporter/Ion Channel Anti-infection Metabolic Enzyme/Protease
  2. Calcium Channel Virus Protease HIV Phosphatase
  3. Ebselen

Ebselen  (Synonyms: SPI-1005; PZ-51; CCG-39161)

Cat. No.: HY-13750 Purity: 99.58%
SDS COA Handling Instructions

Ebselen (SPI-1005), a glutathione peroxidase mimetic, is a potent voltage-dependent calcium channel (VDCC) blocker. Ebselen potently inhibits Mpro (IC50=0.67 μM) and COVID-19 virus (EC50=4.67 μM).Ebselen is an inhibitor of HIV-1 capsid CTD dimerization. Ebselen, an organoselenium compound, can permeate the blood-brain barrier and has anti-inflammatory, antioxidant and anticancer activity.

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

Ebselen Chemical Structure

Ebselen Chemical Structure

CAS No. : 60940-34-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 55 In-stock
Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Solid
5 mg USD 50 In-stock
10 mg USD 70 In-stock
50 mg USD 140 In-stock
100 mg USD 210 In-stock
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Customer Review

Based on 14 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Ebselen purchased from MedChemExpress. Usage Cited in: Exp Ther Med. 2019 Feb;17(2):1412-1419.  [Abstract]

    Ebselen influences the expression of apoptosis‑related proteins. The effects of ebselen on C‑Caspase‑8, C‑Caspase‑3, Bax, Bcl‑2 and C‑PARP are analyzed by western blotting.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Ebselen (SPI-1005), a glutathione peroxidase mimetic, is a potent voltage-dependent calcium channel (VDCC) blocker[1][2]. Ebselen potently inhibits Mpro (IC50=0.67 μM) and COVID-19 virus (EC50=4.67 μM)[3].Ebselen is an inhibitor of HIV-1 capsid CTD dimerization. Ebselen, an organoselenium compound, can permeate the blood-brain barrier and has anti-inflammatory, antioxidant and anticancer activity[4][5].

    IC50 & Target

    HIV-1

     

    Cellular Effect
    Cell Line Type Value Description References
    184B5 GI50
    30.1 μM
    Compound: EBS
    Antiproliferative activity against human 184B5 cells after 72 hrs by MTT assay
    Antiproliferative activity against human 184B5 cells after 72 hrs by MTT assay
    [PMID: 30071406]
    A549 IC50
    > 100 μM
    Compound: PZ51
    Antiproliferative activity against human A549 cells assessed as cell viability after 48 hrs by MTT assay
    Antiproliferative activity against human A549 cells assessed as cell viability after 48 hrs by MTT assay
    [PMID: 25817772]
    A549 IC50
    16.8 μM
    Compound: Ebs
    Cytotoxicity in human A549 cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based assay
    Cytotoxicity in human A549 cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based assay
    [PMID: 29584939]
    A549 IC50
    3.75 μM
    Compound: Ebselen
    Antiproliferative activity against human A549 cells after 48 hrs by CCK-8 assay
    Antiproliferative activity against human A549 cells after 48 hrs by CCK-8 assay
    [PMID: 22483583]
    BEAS-2B GI50
    49.5 μM
    Compound: EBS
    Antiproliferative activity against human BEAS2B cells after 72 hrs by MTT assay
    Antiproliferative activity against human BEAS2B cells after 72 hrs by MTT assay
    [PMID: 30071406]
    Bel-7402 IC50
    68.2 μM
    Compound: PZ51
    Antiproliferative activity against human Bel7402 cells assessed as cell viability after 48 hrs by MTT assay
    Antiproliferative activity against human Bel7402 cells assessed as cell viability after 48 hrs by MTT assay
    [PMID: 25817772]
    Calu-1 GI50
    68.6 μM
    Compound: EBS
    Antiproliferative activity against human HTB-54 cells after 72 hrs by MTT assay
    Antiproliferative activity against human HTB-54 cells after 72 hrs by MTT assay
    [PMID: 30071406]
    CCRF-CEM GI50
    57.1 μM
    Compound: EBS
    Antiproliferative activity against human CCRF-CEM cells after 72 hrs by MTT assay
    Antiproliferative activity against human CCRF-CEM cells after 72 hrs by MTT assay
    [PMID: 30071406]
    CHO-K1 EC50
    6.1 μM
    Compound: 7
    Cytotoxicity against CHO-K1 cells by Alamar blue assay
    Cytotoxicity against CHO-K1 cells by Alamar blue assay
    [PMID: 16962325]
    HCT-116 IC50
    50 μM
    Compound: Ebs
    Cytotoxicity in human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based assay
    Cytotoxicity in human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based assay
    [PMID: 29584939]
    HeLa IC50
    78.5 μM
    Compound: PZ51
    Antiproliferative activity against human HeLa cells assessed as cell viability after 48 hrs by MTT assay
    Antiproliferative activity against human HeLa cells assessed as cell viability after 48 hrs by MTT assay
    [PMID: 25817772]
    HT-29 GI50
    > 100 μM
    Compound: EBS
    Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay
    Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay
    [PMID: 30071406]
    HT-29 IC50
    50.4 μM
    Compound: Ebs
    Cytotoxicity in human HT-29 cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based assay
    Cytotoxicity in human HT-29 cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based assay
    [PMID: 29584939]
    MCF7 IC50
    > 100 μM
    Compound: PZ51
    Antiproliferative activity against human MCF7 cells assessed as cell viability after 48 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells assessed as cell viability after 48 hrs by MTT assay
    [PMID: 25817772]
    MCF7 IC50
    15.02 μM
    Compound: Ebselen
    Antiproliferative activity against human MCF7 cells after 48 hrs by CCK-8 assay
    Antiproliferative activity against human MCF7 cells after 48 hrs by CCK-8 assay
    [PMID: 22483583]
    MCF7 GI50
    58.8 μM
    Compound: EBS
    Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
    [PMID: 30071406]
    MDA-MB-231 IC50
    42.3 μM
    Compound: 1, PZ 51, ebselen
    Antiproliferative activity against human MDA231 cells after 72 hrs by MTT assay
    Antiproliferative activity against human MDA231 cells after 72 hrs by MTT assay
    [PMID: 22204902]
    NCI-H1299 IC50
    27.7 μM
    Compound: Ebs
    Cytotoxicity in human NCI-H1299 cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based assay
    Cytotoxicity in human NCI-H1299 cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based assay
    [PMID: 29584939]
    PC-3 GI50
    > 100 μM
    Compound: EBS
    Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
    Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
    [PMID: 30071406]
    U-266 IC50
    40 μM
    Compound: 62
    Anticancer activity against human U-266 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay
    Anticancer activity against human U-266 cells assessed as cell growth inhibition incubated for 24 hrs by MTS assay
    [PMID: 34217061]
    In Vitro

    Ebselen (SPI-1005; 0.4-100 μM; 20-24 hours) shows strong antiviral effects at a concentration of 10 μM treatment in COVID-19 virus infected Vero cells. Ebsele covalently binds to C145 of the catalytic dyad in COVID-19 virus Mpro[3].
    Ebselen inhibits early viral postentry events of the HIV-1 life cycle by impairing the incoming capsid uncoating process[4].
    Ebselen permeates the blood-brain barrier and inhibits endogenous inositol monophosphatase in mouse brain. Ebselen inhibits inositol monophosphatase (IMPase)[5].
    Ebselen inhibits QSOX1 enzymatic activity and suppresses invasion of pancreatic, renal cancer cell lines[6].

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

    RT-PCR[3]

    Cell Line: COVID-19 virus infected Vero cells
    Concentration: 0.4, 1.2, 3.7, 11.1, 33.3, 100 μM
    Incubation Time: 20-24 hours
    Result: Showed strong antiviral effects at a concentration of 10 μM treatment.
    In Vivo

    Ebselen (5, 10 mg/kg; IP) decreases 5-HT2 agonist-induced head twitches in a dose-dependent manner[5].

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

    Animal Model: 20-25 g 10-12 week old male C57Bl6 mice[5]
    Dosage: 5, 10 mg/kg
    Administration: IP
    Result: Decreased 5-HT2 agonist-induced head twitches in a dose-dependent manner.
    Clinical Trial
    Molecular Weight

    274.18

    Formula

    C13H9NOSe

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to green yellow

    SMILES

    O=C1N(C2=CC=CC=C2)[Se]C3=C1C=CC=C3

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (182.36 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 3.6472 mL 18.2361 mL 36.4723 mL
    5 mM 0.7294 mL 3.6472 mL 7.2945 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. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Concentration
    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    C2

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    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 (9.12 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (9.12 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    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).
    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: 99.58%

    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, 1 year; -20°C, 6 months. 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
    DMSO 1 mM 3.6472 mL 18.2361 mL 36.4723 mL 91.1806 mL
    5 mM 0.7294 mL 3.6472 mL 7.2945 mL 18.2361 mL
    10 mM 0.3647 mL 1.8236 mL 3.6472 mL 9.1181 mL
    15 mM 0.2431 mL 1.2157 mL 2.4315 mL 6.0787 mL
    20 mM 0.1824 mL 0.9118 mL 1.8236 mL 4.5590 mL
    25 mM 0.1459 mL 0.7294 mL 1.4589 mL 3.6472 mL
    30 mM 0.1216 mL 0.6079 mL 1.2157 mL 3.0394 mL
    40 mM 0.0912 mL 0.4559 mL 0.9118 mL 2.2795 mL
    50 mM 0.0729 mL 0.3647 mL 0.7294 mL 1.8236 mL
    60 mM 0.0608 mL 0.3039 mL 0.6079 mL 1.5197 mL
    80 mM 0.0456 mL 0.2280 mL 0.4559 mL 1.1398 mL
    100 mM 0.0365 mL 0.1824 mL 0.3647 mL 0.9118 mL
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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.

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