1. Metabolic Enzyme/Protease
    Immunology/Inflammation
    NF-κB
    Apoptosis
  2. Reactive Oxygen Species
    Apoptosis
  3. Elesclomol

Elesclomol  (Synonyms: STA-4783)

Cat. No.: HY-12040 Purity: 99.40%
COA Handling Instructions

Elesclomol (STA-4783) is a potent copper ionophore and promotes copper-dependent cell death (cuproptosis). Elesclomol specifically binds ferredoxin 1 (FDX1) α2/α3 helices and β5 strand. Elesclomol inhibits FDX1-mediated Fe-S cluster biosynthesis. Elesclomol is an oxidative stress inducer that induces cancer cell apoptosis. Elesclomol is a reactive oxygen species (ROS) inducer. Elesclomol can be used for Menkes and associated disorders of hereditary copper deficiency research.

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

Elesclomol Chemical Structure

Elesclomol Chemical Structure

CAS No. : 488832-69-5

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10 mM * 1 mL in DMSO USD 73 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 105 In-stock
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50 mg USD 220 In-stock
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100 mg USD 385 In-stock
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Customer Review

Based on 11 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Elesclomol purchased from MCE. Usage Cited in: Biomolecules. 2019 Jul 24;9(8):298.   [Abstract]

    Confocal images of MitoSOX fluorescence intensity in CV-1 cells at the 20-min time point after E:C (elesclomol:copper)- treatment in the presence and absence of the mitochondrial superoxide scavenger MitoTEMPO.
    • Biological Activity

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    Description

    Elesclomol (STA-4783) is a potent copper ionophore and promotes copper-dependent cell death (cuproptosis). Elesclomol specifically binds ferredoxin 1 (FDX1) α2/α3 helices and β5 strand. Elesclomol inhibits FDX1-mediated Fe-S cluster biosynthesis. Elesclomol is an oxidative stress inducer that induces cancer cell apoptosis. Elesclomol is a reactive oxygen species (ROS) inducer. Elesclomol can be used for Menkes and associated disorders of hereditary copper deficiency research[1][2][3][4].

    In Vitro

    Elesclomol (STA-4783) binds the FDX1 α2/α3 helices and β5 strand, but does not bind the paralog protein FDX2. Elesclomol-Cu(II) is an FDX1 neo-substrate. FDX1 protein binds and reduces the elesclomol-Cu(II) complex[1].
    Elesclomol-Cu (1:1 ratio) (40 nM) for only 2 hours results in a 15- to 60-fold increase in intracellular copper levels that triggered cell death more than 24 hours later in ABC1 cells[1].
    The addition of copper to elesclomol at a 1:1 molar ratio prior to treatment significantly reduces cell viability when cells are grown in glycolytic (glucose media) conditions[2].
    Elesclomol (200 nM; 18 hours) treatment increases the number of early and late apoptotic cells in HSB2 cells. Elesclomol induces apoptosis in cancer cells through the induction of oxidative stress[3].
    Elesclomol significantly inhibits the cell viability of SK-MEL-5, MCF-7, and HL-60 cells with IC50 values of 110 nM, 24 nM and 9 nM, respectively[5].

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

    Apoptosis Analysis[3]

    Cell Line: HSB2 cells
    Concentration: 200 nM
    Incubation Time: 18 hours
    Result: Increased the number of early and late apoptotic cells.
    In Vivo

    Elesclomol (10 mg/kg; subcutaneous injection; every three days from post-natal day 5 to 26 and once weekly until post-natal day 54) treatment ameliorates severe cardiac pathology with a partial reduction in hypertrophy. Cardiac [Cu] increased with Elesclomol treatment from a vehicle knockout level of 34 to 55%[4].
    Elesclomol escorted copper to the mitochondria and increased cytochrome c oxidase levels in the brain. Elesclomol prevents detrimental neurodegenerative changes and improved the survival of the mottled-brindled mouse[4].

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

    Animal Model: Cardiac Ctr1 knockout mice[4]
    Dosage: 10 mg/kg
    Administration: Subcutaneous injection; every three days from post-natal day 5 to 26 and once weekly until post-natal day 54
    Result: Ameliorated severe cardiac pathology with a partial reduction in hypertrophy.
    Clinical Trial
    Molecular Weight

    400.52

    Formula

    C19H20N4O2S2

    CAS No.
    SMILES

    S=C(C1=CC=CC=C1)N(NC(CC(NN(C(C2=CC=CC=C2)=S)C)=O)=O)C

    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 : 100 mg/mL (249.68 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4968 mL 12.4838 mL 24.9675 mL
    5 mM 0.4994 mL 2.4968 mL 4.9935 mL
    10 mM 0.2497 mL 1.2484 mL 2.4968 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  50% PEG300    50% saline

      Solubility: 5 mg/mL (12.48 mM); Suspended solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (6.24 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (6.24 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.80%

    References
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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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    Product Name:
    Elesclomol
    Cat. No.:
    HY-12040
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