Home Tools
Log in
Cart

Elesclomol

Catalog No. T6170   CAS 488832-69-5
Synonyms: STA-4783

Elesclomol (STA-4783) is an oxidative stress inducer and a highly lipophilic copper ion carrier. Elesclomol induces apoptosis in tumor cells and is used in copper death related studies. Elesclomol also inhibits FDX1-mediated Fe-S cluster biosynthesis.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Elesclomol Chemical Structure
Elesclomol, CAS 488832-69-5
Pack Size Availability Price/USD Quantity
5 mg In stock $ 34.00
10 mg In stock $ 59.00
25 mg In stock $ 94.00
50 mg In stock $ 128.00
100 mg In stock $ 163.00
200 mg In stock $ 243.00
1 mL * 10 mM (in DMSO) In stock $ 39.00
Bulk Inquiry
Get quote
Select Batch  
Purity: 99.51%
Purity: 99.46%
Purity: 99.33%
Contact us for more batch information
Biological Description
Chemical Properties
Storage & Solubility Information
Description Elesclomol (STA-4783) is an oxidative stress inducer and a highly lipophilic copper ion carrier. Elesclomol induces apoptosis in tumor cells and is used in copper death related studies. Elesclomol also inhibits FDX1-mediated Fe-S cluster biosynthesis.
In vitro In nude mouse models carrying human breast cancer (MDA435, MCF7, and ZR-75-1), lung cancer (RER), or lymphoma (U937), Elesclomol ([25-100 mg/kg]) alone demonstrated no anticancer activity. However, it significantly enhanced the efficacy of chemotherapeutic agents such as paclitaxel, leading to tumor regression and extended lifespan in mice.
In vivo Elesclomol exhibits significant inhibitory effects on the viability of SK-MEL-5, MCF-7, and HL-60 cells with IC50 values of 110, 24, and 9 nM, respectively. It induces the production of copper-dependent reactive oxygen species (ROS) and toxicity in yeast cells not by targeting specific intracellular sites but through interaction with the electron transport chain, which leads to elevated levels of ROS in organelles and consequently, cell death. Furthermore, treatment with 100 nM Elesclomol significantly induces the expression of heat shock response genes and metallothionein genes in Hs294T cells as analyzed through Affymetrix gene chip at 6 hours post-treatment. In Ramos Burkitt's lymphoma B cells treated with 100 nM Elesclomol, Hsp70 RNA levels increase by 4.8-fold and 160-fold after 1 and 6 hours, respectively. Additionally, ROS levels rise by 20% and 385% after 0.5 and 6 hours of treatment, with antioxidant pretreatments like N-acetylcysteine and Tiron inhibiting the induction of Hsp70. Treatment with 200 nM Elesclomol for 18 hours increases early and late apoptosis in HSB2 cells by 3.7 and 11 times, respectively, through the induction of oxidative stress.
Kinase Assay In vitro enzyme assays for PLK1: Recombinant PLK1 (10 ng) is incubated with different concentrations of Rigosertib in a 15 μL reaction mixture (50 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 2 mM Dithiothreitol, 0.01% NP-40 [pH 7.5]) for 30 min at room temperature. Kinase reactions are performed for 20 min at 30 °C in a volume of 20 μL (15 μL enzyme + inhibitor, 2 μL 1 mM ATP), 2 μL of γ32P-ATP (40 μCi), and 1 μL of recombinant Cdc25C (100 ng) or casein (1 μg) substrates. Reactions are terminated by boiling for 2 min in 20 μL of 2× Laemmli buffer. Phosphorylated substrates are separated by 18% SDS-PAGE. The gels are dried and exposed to X-ray film for 3-10 min.
Cell Research Cells are treated with various concentrations of Elesclomol for 18 or 24 hours. The level of intracellular ROS is monitored using the DCFDA probe, which emits a green fluorescence on oxidation. Cell death is determined by flow cytometry of cells double stained with Annexin V/FITC and propidium iodide (PI) using a Vybrant Apoptosis assay kit.(Only for Reference)
Synonyms STA-4783
Molecular Weight 400.52
Formula C19H20N4O2S2
CAS No. 488832-69-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 74 mg/mL (184.8 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Bair JS, et al. Chemistry and biology of deoxynyboquinone, a potent inducer of cancer cell death. J Am Chem Soc. 2010 Apr 21;132(15):5469-78. 2. Kirshner JR, et al. Elesclomol induces cancer cell apoptosis through oxidative stress. Mol Cancer Ther. 2008 Aug;7(8):2319-27. 3. Modica-Napolitano JS, et al. The Anticancer Agent Elesclomol Has Direct Effects on Mitochondrial Bioenergetic Function in Isolated Mammalian Mitochondria. Biomolecules. 2019 Jul 24;9(8):298. 4. Lee JH, et al. Genipin enhances the antitumor effect of elesclomol in A549 lung cancer cells by blocking uncoupling protein-2 and stimulating reactive oxygen species production. Oncol Lett. 2020 Dec;20(6):374. 5. Yuan S, et al. Oral Elesclomol Treatment Alleviates Copper Deficiency in Animal Models. Front Cell Dev Biol. 2022 Apr 1;10:856300.

TargetMolCitations

1. Wu Z, Lin C, Zhang F, et al.TIGD1 Function as a Potential Cuproptosis Regulator Following a Novel Cuproptosis-Related Gene Risk Signature in Colorectal Cancer.Cancers.2023, 15(8): 2286.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Cuproptosis Compound Library Anti-Obesity Compound Library ReFRAME Related Library Ferroptosis Compound Library Endoplasmic Reticulum Stress Compound Library

Related Products

Related compounds with same targets
Physalin B Nevanimibe hydrochloride FLLL32 Enpp/Carbonic anhydrase-IN-2 Caudatin Tubastatin A Amuvatinib Lonicerin

TargetMolDose Conversion

You can also refer to dose conversion for different animals. More

TargetMol In vivo Formulation Calculator (Clear solution)

Step One: Enter information below
Dosage
mg/kg
Average weight of animals
g
Dosing volume per animal
ul
Number of animals
Step Two: Enter the in vivo formulation
% DMSO
%
% Tween 80
% ddH2O
Calculate Reset

TargetMolCalculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator
=
X
X

Molarity Calculator allows you to calculate the

  • Mass of a compound required to prepare a solution of known volume and concentration
  • Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

X
=
X

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

=
/

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Elesclomol 488832-69-5 Apoptosis Cytoskeletal Signaling Immunology/Inflammation Metabolism NF-Κb HSP Reactive Oxygen Species copper ionophore ferredoxin 1 ROS hereditary copper Inhibitor FDX1 cancer Menkes Fe-S cluster Cuproptosis β5 strand α2/α3 helices STA-4783 STA 4783 copper oxidative stress STA4783 inhibit inhibitor

 

TargetMol