2. Apoptosis Anti-infection
  3. Apoptosis Bacterial
  4. AMXT-1501

AMXT-1501 is a Bacterial agent and polyamine transport system inhibitor. AMXT-1501 targets membrane phospholipids and exhibits antibacterial activity against a variety of Gram-positive and Gram-negative multidrug-resistant bacteria. AMXT-1501 inhibits capsular biosynthesis in Streptococcus pneumoniae. AMXT-1501 targets ornithine decarboxylase and polyamines to inhibit the proliferation of neuroblastoma cells. AMXT-1501 in combination with DFMO (HY-B0744) induces Apoptosis in neuroblastoma cells. AMXT-1501 is applicable to research related to multidrug-resistant bacterial infections, pneumococcal infections, Streptococcus pneumoniae infections, and neuroblastoma.

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

CAS No. : 441022-64-6

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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of AMXT-1501:

AMXT-1501 Related Antibodies

Top Publications Citing Use of Products

    AMXT-1501 purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2024 Jul;31(7):910-923.  [Abstract]

    IC50s of AMXT-1501 (4, 8, 12, 16, 20, 24 μM) in CLB-BAR, CLB-GE, SK-N-BE(2) and SH-SY5Y cells after 5 d treatment.

    AMXT-1501 purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2024 Jul;31(7):910-923.  [Abstract]

    Immunoblot analysis of neuronal differentiation markers (RET and DLG2) in SK-N-BE(2) and SH-SY5Y cells treated with AMXT-1501 (0 or 8 µM) and RA (0 or 5 µM) for 48 h or 24 h .

    AMXT-1501 purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2024 Jul;31(7):910-923.  [Abstract]

    Cells after AMXT-1501 (0 or 8 µM) and RA (0 or 5 µM) treatment as indicated for 48 h or 24 h.

    AMXT-1501 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2024 Nov 17:2024.08.24.609500.

    Representative fluorescence images of cells upon indicated treatments. AMXT-1501 (0.5 μM; polyamine import inhibitor), DFMO (1 mM), and spermidine (5 μM).

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    AMXT-1501 is a Bacterial agent and polyamine transport system inhibitor. AMXT-1501 targets membrane phospholipids and exhibits antibacterial activity against a variety of Gram-positive and Gram-negative multidrug-resistant bacteria. AMXT-1501 inhibits capsular biosynthesis in Streptococcus pneumoniae. AMXT-1501 targets ornithine decarboxylase and polyamines to inhibit the proliferation of neuroblastoma cells. AMXT-1501 in combination with DFMO (HY-B0744) induces Apoptosis in neuroblastoma cells. AMXT-1501 is applicable to research related to multidrug-resistant bacterial infections, pneumococcal infections, Streptococcus pneumoniae infections, and neuroblastoma[1][2][3][4].

    IC50 & Target

    Polyamine transport[1]
    Cellular Effect
    Cell Line Type Value Description References
    MDA-MB-231 IC50
    57 μM
    Compound: 11, D-Lys(C(16)acyl)-Spm
    Cytotoxicity against human MDA-MB-231 cells after 6 days by MTS/PMS dye assay
    Cytotoxicity against human MDA-MB-231 cells after 6 days by MTS/PMS dye assay
    		[PMID: 19281226]
    In Vitro

    AMXT-1501 (1.56-50 μM) exhibits dose-dependent antibacterial activity against a variety of Gram-positive and Gram-negative multidrug-resistant (MDR) bacterial isolates, with MIC50/MIC90 values ranging from 3.13 to 12.5 μM[1].
    AMXT-1501 (8× MIC; 0-24 h) exhibits rapid and potent bactericidal activity against planktonic MRSA, ESBL-producing E. coli, and CR E. coli[1].
    AMXT-1501 (1-4× MIC; 0.5-24 h) reduces biofilm formation in a dose-dependent manner in most tested Staphylococcus aureus (MSSA and MRSA) and Enterococcus faecalis strains, causes severe damage to the cell membranes of MRSA and CR E. coli, increases membrane permeability and depolarizes them, thereby leading to bacterial cell death[1].
    AMXT-1501 (3.125-50 μg/mL; 90 s) binds directly to the bacterial membrane phospholipids CL and PG[1].
    AMXT-1501 (7.4 μM; cultured until OD600 reaches 0.2-0.5) inhibits capsular polysaccharide biosynthesis by 61% in Streptococcus pneumoniae serotype 2 (strain D39), depletes intracellular polyamines and glucuronic acid, and simultaneously increases intracellular glucose levels[2].
    AMXT-1501 (7.4 μM) regulates gene expression in Streptococcus pneumoniae D39, thereby enhancing the biosynthesis of polyamines and glucose, inhibiting ATP production and fatty acid synthesis, and upregulating stress response pathways[3].
    AMXT-1501 (0.39-50 μM; 48 h) potently inhibits the viability of human neuroblastoma cell lines BE (2)-C, SMS-KCNR and SH-SY5Y in vitro, with IC50 values of 17.69 μM, 17.72 μM and 14.13 μM, respectively[4].
    AMXT-1501 (2.5 μM; 96 h) induced apoptosis in BE (2)-C, SMS-KCNR and SH-SY5Y human neuroblastoma cells when used in combination with DFMO[4].

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

    AMXT-1501 Related Antibodies

    Cell Cytotoxicity Assay[4]

    Cell Line: BE(2)-C, SMS-KCNR, SH-SY5Y
    Concentration: 0.39-50 μM
    Incubation Time: 48 h
    Result: Induced cytotoxicity with IC50 values of 17.69 μM (BE(2)-C), 17.72 μM (SMS-KCNR), and 14.13 μM (SH-SY5Y).

    Apoptosis Analysis[4]

    Cell Line: BE(2)-C, SMS-KCNR, SH-SY5Y
    Concentration: 2.5 μM+2.5 mM DFMO
    Incubation Time: 96 h
    Result: Induced apoptosis.
    Reduced the amount of uncleaved PARP and increased the amounts of cleaved PARP and cleaved caspase-3.
    In Vivo

    AMXT-1501 (20 mg/kg; i.p.; every 12 h; 3 days) significantly reduces the size of skin abscesses and decreases MRSA loads in BALB/c mice[1].
    AMXT-1501 (20 mg/kg; i.p.; every 12 h; 3 days) significantly improves the survival rate of BALB/c mice with bacterial abdominal infection and reduces the bacterial load of CRE E. coli in their lung and liver tissues[1].

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

    Animal Model: BALB/c (female, 6-8-week-old, 18-22 g) (S. aureus YUSA145 (MRSA)(1×107 CFU))[1]
    Dosage: 20 mg/kg
    Administration: i.p.; every 12 h; 3 days
    Result: Reduced skin abscess areas significantly.
    Lowered bacterial loads in abscess tissue (log10 CFU/g) significantly.
    Animal Model: BALB/c (female, 6-8-week-old, 18-22 g) (E. coli ECO2219 (CRE)(2×109 CFU))[1]
    Dosage: 20 mg/kg
    Administration: i.p.; every 12 h; 3 days
    Result: Achieved a 50% survival rate through day 7, which was higher than the survival rate in tigecycline-treated mice.
    Lowered bacterial loads in lung tissue (log10 CFU/g) significantly.
    Lowered bacterial loads in liver tissue (log10 CFU/g) significantly.
    Clinical Trial
    Molecular Weight

    568.92

    Formula

    C32H68N6O2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CCCCCCCCCCCCCCCC(NCCCC[C@@H](N)C(NCCCNCCCCNCCCN)=O)=O
    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: 

    H2O : 100 mg/mL (175.77 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7577 mL 8.7886 mL 17.5772 mL
    5 mM 0.3515 mL 1.7577 mL 3.5154 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.

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

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    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
    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 1 mM 1.7577 mL 8.7886 mL 17.5772 mL 43.9429 mL
    5 mM 0.3515 mL 1.7577 mL 3.5154 mL 8.7886 mL
    10 mM 0.1758 mL 0.8789 mL 1.7577 mL 4.3943 mL
    15 mM 0.1172 mL 0.5859 mL 1.1718 mL 2.9295 mL
    20 mM 0.0879 mL 0.4394 mL 0.8789 mL 2.1971 mL
    25 mM 0.0703 mL 0.3515 mL 0.7031 mL 1.7577 mL
    30 mM 0.0586 mL 0.2930 mL 0.5859 mL 1.4648 mL
    40 mM 0.0439 mL 0.2197 mL 0.4394 mL 1.0986 mL
    50 mM 0.0352 mL 0.1758 mL 0.3515 mL 0.8789 mL
    60 mM 0.0293 mL 0.1465 mL 0.2930 mL 0.7324 mL
    80 mM 0.0220 mL 0.1099 mL 0.2197 mL 0.5493 mL
    100 mM 0.0176 mL 0.0879 mL 0.1758 mL 0.4394 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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    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:

    AMXT-1501441022-64-6AMXT1501AMXT 1501ApoptosisBacterialbacterial agentpolyamine transport system inhibitorE. coliEnterococcus faecalisStaphylococcus aureusBE (2)-C cellsSMS-KCNR cellsSH-SY5Ycellsmultidrug-resistant bacterial infectionspneumococcal infectionsStreptococcus pneumoniae infectionsneuroblastoma
    Inhibitorinhibitorinhibit

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