1. Anti-infection Metabolic Enzyme/Protease Apoptosis
  2. Aminopeptidase Bacterial MMP Apoptosis Antibiotic
  3. Actinonin

Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities.

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

CAS No. : 13434-13-4

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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Actinonin:

Top Publications Citing Use of Products

    Actinonin purchased from MedChemExpress. Usage Cited in: Sci Rep. 2024 Jun 28;14(1):14900.  [Abstract]

    The growth of vector alone and EcPDF3f SW480 cells in the absence or presence of Actinonin (5 µg/ml final concentration).

    Actinonin purchased from MedChemExpress. Usage Cited in: Sci Rep. 2024 Jun 28;14(1):14900.  [Abstract]

    Immunoblotting of SOX2 in control and EcPDF3f SW480 cells with or without Actinonin (2 µg/ml) treatment for 2 days.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities[1][2][3][4][5].

    IC50 & Target

    Ki: 0.28 nM (Peptide deformylase (PDF))[2], 300 nM (MMP-1), 1,700 nM (MMP-3), 190 nM (MMP-8), 330 nM (MMP-9)[3], and 20 nM (hmeprin α)[5]
    Apoptosis[1]
    Aminopeptidase M, Aminopeptidase N and Leucine aminopeptidase[1]

    Cellular Effect
    Cell Line Type Value Description References
    BMDM CC50
    > 193 μg/mL
    Compound: Actinonin
    Cytotoxicity against mouse BMDM cells
    Cytotoxicity against mouse BMDM cells
    [PMID: 35307568]
    BMDM CC50
    > 500 μM
    Compound: Actinonin
    Cytotoxicity against mouse BMDM cells
    Cytotoxicity against mouse BMDM cells
    [PMID: 35307568]
    HCT-116 IC50
    22.6 μM
    Compound: Actinonin
    Antiproliferative activity against human HCT116 cells assessed as reduction in cell growth measured after 48 hrs by CCK8 assay
    Antiproliferative activity against human HCT116 cells assessed as reduction in cell growth measured after 48 hrs by CCK8 assay
    [PMID: 32551649]
    HEK293 IC50
    15 μM
    Compound: 1
    Cytotoxicity against human HEK293 cells
    Cytotoxicity against human HEK293 cells
    [PMID: 21719286]
    HL-60 IC50
    100 μM
    Compound: 1
    Cytotoxicity against human vincristine-resistant HL60 cells
    Cytotoxicity against human vincristine-resistant HL60 cells
    [PMID: 21719286]
    HL-60 IC50
    16 μM
    Compound: 1
    Cytotoxicity against human HL60 cells
    Cytotoxicity against human HL60 cells
    [PMID: 21719286]
    Jurkat IC50
    40 μM
    Compound: 1
    Cytotoxicity against human Jurkat cells
    Cytotoxicity against human Jurkat cells
    [PMID: 21719286]
    MOLT-3 IC50
    45 μM
    Compound: 1
    Cytotoxicity against human MOLT3 cells
    Cytotoxicity against human MOLT3 cells
    [PMID: 21719286]
    In Vitro

    Actinonin inhibits cell growth in various human tumor cell lines. The IC50 of 4, 6.9, 12.8, 16.6, 27.4, 15.7 and 49.3 μM for Raji cells, MDA-MB-468 cells,PC3 cells, SK-LC-19 cells, Hela cells, HT-1080 cells and AL67 cells, respectively[1].
    HsPDF is a critical target of actinonin and that the inhibition of this protein in the mitochondria leads to cell death in tumor cells. Actinonin treatment of cells led to a tumor-specific mitochondrial membrane depolarization and ATP depletion in a time- and dose-dependent manner[1].
    Actinonin is a potent inhibitor of all three forms (Zn-, Ni-, and Fe-) of peptide deformylases from both S. aureus and E. coli bacteria. Under the assay conditions, the IC50 values for Actinonin are 90, 3, 0.8, and 11 nM for Zn-PDF (E. coli), Ni-PDF (E. coli), Fe-PDF (E. coli), and Ni-PDF (S. aureus), respectively[2].
    Actinonin is active against Gram-positive bacteria, including S. aureus (MIC value of 8-16 μg/mL), Streptococcus pyogenes (MIC value of 8 μg/mL) and Streptococcus epidermidis (MIC value of 2-4 μg/mL). Actinonin is also active against fastidious Gramne-gative bacteria, such as H. influenzae (MIC value of 1-2 μg/mL), Moraxella catarrhalis (MIC value of 0.5 μg/mL), and Neisseria gonorrheae (MIC value of 1-4 μg/mL). Actinonin is very active against the H. influenzae acr (MIC value of 0.13 μg/mL) and E. coli acr (MIC value of 0.25 μg/mL) efflux pump mutants[2].

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

    In Vivo

    Actinonin has been safely administered to mice as an antibiotic at doses up to 400 mg/kg. Actinonin does not appear to have significant toxicity to normal tissues, despite its antitumor activity in vitro. Remarkably, Actinonin exhibits significant antitumor activity when given i.p. or orally in a CWR22 human prostate tumor xenograft model in nude mice. During treatment, the animals show no signs of toxicity[1].

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

    Molecular Weight

    385.50

    Formula

    C19H35N3O5

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(N[C@H](C(N1[C@H](CO)CCC1)=O)C(C)C)[C@H](CCCCC)CC(NO)=O

    Structure Classification
    Initial Source
    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 (129.70 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 2.5940 mL 12.9702 mL 25.9403 mL
    5 mM 0.5188 mL 2.5940 mL 5.1881 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.

    • 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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    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: ≥ 5 mg/mL (12.97 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: 5 mg/mL (12.97 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: 98.37%

    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 2.5940 mL 12.9702 mL 25.9403 mL 64.8508 mL
    5 mM 0.5188 mL 2.5940 mL 5.1881 mL 12.9702 mL
    10 mM 0.2594 mL 1.2970 mL 2.5940 mL 6.4851 mL
    15 mM 0.1729 mL 0.8647 mL 1.7294 mL 4.3234 mL
    20 mM 0.1297 mL 0.6485 mL 1.2970 mL 3.2425 mL
    25 mM 0.1038 mL 0.5188 mL 1.0376 mL 2.5940 mL
    30 mM 0.0865 mL 0.4323 mL 0.8647 mL 2.1617 mL
    40 mM 0.0649 mL 0.3243 mL 0.6485 mL 1.6213 mL
    50 mM 0.0519 mL 0.2594 mL 0.5188 mL 1.2970 mL
    60 mM 0.0432 mL 0.2162 mL 0.4323 mL 1.0808 mL
    80 mM 0.0324 mL 0.1621 mL 0.3243 mL 0.8106 mL
    100 mM 0.0259 mL 0.1297 mL 0.2594 mL 0.6485 mL
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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.

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