Elesclomol (STA-4783)

Alias: STA 4783, Elesclomol; STA4783; STA-4783;
Cat No.:V0876 Purity: ≥98%
Elesclomol (STA4783; STA-4783;STA4783) is a bis(thio-hydrazide amide)-basedheat shock protein 70/HSP70induceras well as anoxidative stress inducer with potential antitumor and pro-apoptotic activity.
Elesclomol (STA-4783) Chemical Structure CAS No.: 488832-69-5
Product category: HSP
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
250mg
500mg
Other Sizes
Official Supplier of:
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text

 

  • Business Relationship with 5000+ Clients Globally
  • Major Universities, Research Institutions, Biotech & Pharma
  • Citations by Top Journals: Nature, Cell, Science, etc.
Top Publications Citing lnvivochem Products
Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Elesclomol (STA4783; STA-4783; STA4783) is a bis(thio-hydrazide amide)-based heat shock protein 70/HSP70 inducer as well as an oxidative stress inducer with potential antitumor and pro-apoptotic activity. It activates natural killer (NK) cell-mediated tumor killing and elicits pro-apoptosis events among tumor cells. It was developed by GSK company as a chemotherapy adjuvant but the trial was suspended due to safety concerns.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
FDX1's α2/α3 helix and β5 strand are bound by elisclomol (STA-4783), but not by the paralogous protein FDX2. A novel FDX1 substrate is elesclomol-Cu(II). Elesclomol-Cu(II) complex is bound by and reduced by the FDX1 protein [1]. After just two hours, electrolysomol-Cu (1:1 ratio) (40 nM) increases intracellular copper levels by 15–60 times, leading to the death of ABC1 cells within 24 hours [1]. Prior to treatment, adding copper to elesclomol at a 1:1 molar ratio dramatically lowers cell viability in cells grown in glycolytic (glucose media) culture [2]. HSB2 cells treated with esclomol (200 nM; 18 hours) have more early and late apoptotic cells. Elesclomol causes oxidative stress, which causes cancer cells to undergo apoptosis [3]. Elesclomol, with IC50 values of 110 nM, 24 nM, and 9 nM, respectively, dramatically reduces the viability of SK-MEL-5, MCF-7, and HL-60 cells [5].
ln Vivo
Elesclomol (10 mg/kg; subcutaneous; every three days from postpartum day 5 to 26 and weekly till postpartum day 54) treatment improved hypertrophic heart disease and partially decreased severe cardiac pathology. After receiving Elesclomol, heart [Cu] rose from 34% to 55% of vector knockout levels [4]. Elesclomol raises the amounts of cytochrome c oxidase in the brain and transports copper to the mitochondria. In spotted mice, eloxamol enhances survival and averts detrimental neurological alterations [4].
Cell Assay
Apoptosis Analysis[3]
Cell Types: HSB2 cells
Tested Concentrations: 200 nM
Incubation Duration: 18 hrs (hours)
Experimental Results: Increased the number of early and late apoptotic cells.
Animal Protocol
Animal/Disease Models: Cardiac Ctr1 knockout mice[4]
Doses: 10 mg/kg
Route of Administration: subcutaneous (sc) injection; every three days from post-natal day 5 to 26 and once weekly until post-natal day 54
Experimental Results: Ameliorated severe cardiac pathology with a partial reduction in hypertrophy.
References
[1]. Peter Tsvetkov, et al. Copper induces cell death by targeting lipoylated TCA cycle proteins. Science. 2022 Mar 18;375(6586):1254-1261.
[2]. Peter Tsvetkov, et al. Mitochondrial metabolism promotes adaptation to proteotoxic stress. Nat Chem Biol. 2019 Jul;15(7):681-689.
[3]. Kirshner JR, et al. Elesclomol induces cancer cell apoptosis through oxidative stress. Mol Cancer Ther. 2008 Aug;7(8):2319-27.
[4]. Liam M Guthrie, et al. Elesclomol alleviates Menkes pathology and mortality by escorting Cu to cuproenzymes in mice. Science. 2020 May 8;368(6491):620-625.
[5]. 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):5469-7
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H20N4O2S2
Molecular Weight
400.5
CAS #
488832-69-5
SMILES
O=C(NN(C)C(C1=CC=CC=C1)=S)CC(NN(C)C(C2=CC=CC=C2)=S)=O
InChi Key
BKJIXTWSNXCKJH-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H20N4O2S2/c1-22(18(26)14-9-5-3-6-10-14)20-16(24)13-17(25)21-23(2)19(27)15-11-7-4-8-12-15/h3-12H,13H2,1-2H3,(H,20,24)(H,21,25)
Chemical Name
N'1,N'3-dimethyl-N'1,N'3-di(phenylcarbonothioyl)malonohydrazide
Synonyms
STA 4783, Elesclomol; STA4783; STA-4783;
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 80 mg/mL (199.8 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Solubility (In Vivo)
1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.4969 mL 12.4844 mL 24.9688 mL
5 mM 0.4994 mL 2.4969 mL 4.9938 mL
10 mM 0.2497 mL 1.2484 mL 2.4969 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in 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.
/

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
+
+
+

Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • Elesclomol (STA-4783)

    Elesclomol induces oxidative stress.



    Elesclomol (STA-4783)

    Elesclomol induces ROS and Hsp70 RNA at early times.Mol Cancer Ther.2008 Aug;7(8):2319-27.
  • Elesclomol (STA-4783)

    Elesclomol induces Hsp70 RNA via oxidative stress.Mol Cancer Ther.2008 Aug;7(8):2319-27.
  • Elesclomol (STA-4783)

    Oxidative stress mediates elesclomol-induced apoptosis.Mol Cancer Ther.2008 Aug;7(8):2319-27.
Contact Us