EMD638683

Catalog No.S8824 Batch:S882402

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Technical Data

Formula

C18H18F2N2O4

Molecular Weight 364.34 CAS No. 1181770-72-8
Solubility (25°C)* In vitro DMSO 73 mg/mL (200.36 mM)
Ethanol 73 mg/mL (200.36 mM)
Water Insoluble
* <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.)

Preparing Stock Solutions

Biological Activity

Description EMD638683 is a highly selective inhibitor of serum- and glucocorticoid-inducible kinase 1 (SGK1) with IC50 of 3 μM. EMD638683 exhibits antihypertensive potency and anti-tumor activity.
Targets
SGK1 [1]
(Cell-free assay)
3 μM
In vitro

In vitro testing discloses EMD638683 as a SGK1 inhibitor with an IC50 of 3 μM.[1] EMD638683 treatment significantly augments the radiation‑induced decrease of forward scatter, increase of phosphatidylserine exposure, decrease of mitochondrial potential, increase of caspase 3 activity, increase of DNA fragmentation and increase of late apoptosis.[2]

In vivo

The in vivo development of tumors following chemical carcinogenesis is significantly blunted by treatment with EMD638683.[2] Within 24 hours in vivo EMD638683 treatment significantly decreases blood pressure in fructose/saline-treated mice but not in control animals or in SGK1 knockout mice.[1]

Protocol (from reference)

Cell Assay:

[1]

  • Cell lines

    HeLa-cells

  • Concentrations

    0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM

  • Incubation Time

    24 h

  • Method

    The cells are plated in 6-wells MTPs at a density of 10–20 × 103 cells/cm2 in Dulbecco´s DMEM medium, supplemented with 10% fetal calf serum (FCS), 2 mM glutamine and 1 mM sodium pyruvate. After 24 hrs at 37℃ and 5% CO2 in a cell incubator, each well is further supplemented with 25 μl of a 100X dimethyl sulfoxide (DMSO) solution of the compound; the solution is diluted 100-fold in the supernatant of the cell culture, thus resulting in the anticipated SGK1-inhibitor concentration at a 1% DMSO concentration.

Animal Study:

[2]

  • Animal Models

    8-week-old wild type mice

  • Dosages

    20 mg/kg, 600 mg/kg

  • Administration

    IP, Oral gavage

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.