Diethylmaleate

Catalog No.S4712 Batch:S471202

Technical Data

Formula

C₈H₁₂O₄

Molecular Weight

172.18

CAS No.

141-05-9

Solubility (25°C)*

In vitro

In vivo (Add solvents to the product individually and in order)

Clear solution

5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O

5.0mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Biological Activity

Description

Diethylmaleate (Diethyl ester, Maleic acid diethyl ester) is the diethyl ester of maleic acid and a glutathione-depleting compound that inhibits NF-κB.

Targets

NF-κB ^[5]

Nrf2 ^[3]

In vitro

DEM induces upregulation of GSH(L-c-glutamyl-L-cysteinyl-glycine) metabolism, and the downregulation of pathways of cancer, chemokine signaling, cytokine-cytokine receptor, and focal adhesion in transformed cells. DEM appears to modify microenvironment of transformed cells thereby restraining tumor cell growth. DEM is cytotoxic to the transformed cells in a concentration dependent manner. DEM at 0.25 mM decreases cell viability to 75%. The co-exposure of cells to DEM+GSHe inhibits DEM induced cytotoxicity. DEM exposure increases the ROS generation by multiple orders of magnitude in transformed cells. This is evident from the dose and time dependent increase in fluorescence intensity of CMH2DCFDA. Moreover, DEM activates MAPK pathway and DEM induced activation of ERK is found to be due to phosphorylation at Thr 202/204^[1].

In vivo

Sperm motility and epididymal sperm count are significantly reduced in the DEM treated animals. Fertility status is also affected by DEM exposure as is evident from the percent fertility and the litter size. consequences of the oxidative stress produced by the DEM induces glutathione depletion, on the reproductive ability of male mice and modulation of the various components of the antioxidant defense system at the transcriptional level^[4].

Density

1.064 g/mL at 25 °C

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines Transformed cells (tC3H10T1/2 and tBALB/c) Concentrations Various test concentrations (0.05-1 mM) Incubation Time 24 h Method A stock solution of DEM is prepared in 100% DMSO and diluted in DMEM to achieve the desired concentration with less than 0.1% DMSO in the culture wells. Briefly, cells are seeded (1 ×10⁴ cells/well) in 96-well plates and allowed to adhere overnight. Subsequently, these cells are exposed to DEM at various test concentrations (0.05-1 mM) or co-exposed to equimolar (0.25 mM) DEM+GSHe for 24 h. Cell viability is determined by recording the OD at 570 nm in an Elisa microplate reader.
Animal Study:^{^[2]}	Animal Models Sprague-Dawley rats Dosages A range of doses up to a maximum of 6mmol/kg Administration i.p

Cell Assay:^{^[1]}

Cell lines
Transformed cells (tC3H10T1/2 and tBALB/c)
Concentrations
Various test concentrations (0.05-1 mM)
Incubation Time
24 h
Method
A stock solution of DEM is prepared in 100% DMSO and diluted in DMEM to achieve the desired concentration with less than 0.1% DMSO in the culture wells. Briefly, cells are seeded (1 ×10⁴ cells/well) in 96-well plates and allowed to adhere overnight. Subsequently, these cells are exposed to DEM at various test concentrations (0.05-1 mM) or co-exposed to equimolar (0.25 mM) DEM+GSHe for 24 h. Cell viability is determined by recording the OD at 570 nm in an Elisa microplate reader.

Animal Study:^{^[2]}

Animal Models
Sprague-Dawley rats
Dosages
A range of doses up to a maximum of 6mmol/kg
Administration
i.p

References

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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