Home Metabolism SGK inhibitor EMD638683 For research use only.

EMD638683

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.

EMD638683 Chemical Structure

EMD638683 Chemical Structure

CAS: 1181770-72-8

Purity & Quality Control

Batch: Purity: 99.94%
99.94

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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

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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models 8-week-old wild type mice
Dosages 20 mg/kg, 600 mg/kg
Administration IP, Oral gavage

Chemical Information & Solubility

Molecular Weight 364.34 Formula

C18H18F2N2O4
CAS No. 1181770-72-8 SDF --
Smiles CCC1=C(C=CC(=C1C)O)C(=O)NNC(=O)C(C2=CC(=CC(=C2)F)F)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 73 mg/mL ( (200.36 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 73 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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