1. Metabolic Enzyme/Protease
  2. SGK

EMD638683 

Cat. No.: HY-15193 Purity: 99.74%
Data Sheet SDS Handling Instructions

EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM.

For research use only. We do not sell to patients.
EMD638683 Chemical Structure

EMD638683 Chemical Structure

CAS No. : 1181770-72-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO $286 In-stock
5 mg $260 In-stock
10 mg $335 In-stock
50 mg $905 In-stock
100 mg $1500 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of EMD638683:

    EMD638683 purchased from MCE. Usage Cited in: FASEB J. 2015 Sep;29(9):3737-49.

    Phosphorylation of NDRG-1 is completely suppressed by 10 μM EMD638683 in human monocytes upon LPS stimulation. Whole cell lysates of purified human monocytes upon LPS stimulation and EMD638683 pre-treatment are probed for phosphorylation of the SGK1 substrate, NDRG, and total GAPDH by Western Blot.

    EMD638683 purchased from MCE. Usage Cited in: Environ Toxicol Pharmacol. 2014 Sep;38(2):374-8.

    Effects of EMD638683 and SGK1 knockdown on the CdCl2-induced phosphorylation of SGK1, NDRG1, FoxO3a, andCREB in HK-2 cells. Cells are incubated with 50 μM EMD638683 for 1 h and then incubated with or without 20 μM CdCl2 for 8 h.

    EMD638683 purchased from MCE. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2017 Apr 1;49(4):302-310.

    The expression levels of SGK1 at different concentrations of Wogonin and EMD638683 are assayed using western blot with GAPDH as an internal control.

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    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM.

    IC50 & Target

    IC50: 3 μM (SGK1)[1]

    In Vitro

    EMD638683 is a SGK1 inhibitor. EMD638683 inhibits the NDRG1 (N-Myc downstream-regulated gene 1) phosphorylation, an effect requiring 3.35±0.32 μM EMD638683 in the cell culture medium for half maximal effect (IC50). EMD638683 has also an inhibitory effect on cAMP-dependent protein kinase (PKA), mitogen- and stress-activated protein kinase 1 (MSK1), protein kinase C-related kinase 2 (PKR2), and the SGK isoforms SGK2 and SGK3[1]. In both, control and EMD638683 (50 µM)-treated CaCo-2 cells, radiation significantly increases the percentage of CaCo-2 cells undergoing late apoptosis. EMD638683 treatment alone tends to enhance the percentage of apoptotic CaCo-2 cells. Following radiation the percentage of apoptotic EMD638683-treated CaCo-2 cells is significantly higher than the percentage of apoptotic control cells. Thus, EMD638683 treatment significantly augments the apoptosis following radiation[2].

    In Vivo

    The colon is significantly longer and the colon weight significantly lower in EMD638683-treated mice than in placebo-treated mice, a finding pointing to an influence of EMD638683 on tumor growth following chemical carcinogenesis. In addition, the stomach weight is significantly lower in the EMD treated group. Most importantly, the number of developing tumors following carcinogenic treatment is significantly blunted by EMD638683 treatment[2]. EMD638683 (20 mg/kg, intragastrically) prevents progression of monocrotaline (MCT)-induced pulmonary vascular remodeling in rats. Hemodynamic characteristics show that EMD638683 treatment attenuates right ventricular systolic pressure (RVSP) (15.8±2.5 vs. 28.2±3.1 mmHg; P<0.05; n=6) and right ventricular hypertrophy index (RVHI) (0.27±0.02 vs. 0.41±0.06;P<0.05; n=6) compare to vehicle-dosed controls[3].

    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
    1 mM 2.7447 mL 13.7234 mL 27.4469 mL
    5 mM 0.5489 mL 2.7447 mL 5.4894 mL
    10 mM 0.2745 mL 1.3723 mL 2.7447 mL
    Cell Assay
    [2]

    EMD638683 is dissolved in DMSO and stored, and then diluted with appropriate media before use[2].

    Colon carcinoma (CaCo-2) cells are grown in complete DMEM medium containing 10% fetal calf serum, 1% sodium pyruvate, 1% penicillin-streptomycin and 1% non-essential amino acids under standard culture conditions (37°C, 5% CO2). 105 cells are seeded in 6 well plates and cultured with fresh culture medium for 24 h, after which EMD638683 (50 µM) is applied for 24 hours. For comparison, the cells are treated with the solvent (0.2 μL DMSO) and one solvent control is analysed with each set of experiments. The cells are subsequently exposed to 3.18 min radiation (3 Gray). After further incubation for 72 h in the presence or absence of EMD638683 (50 µM) the cells are analyzed utilizing flow cytometry[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    EMD638683 is synthesized by Haoyuan (Shanghai, China) and dissolved in 1 % DMSO[3].

    Rat and Mice[3]
    PAH is induced in 2-month-old male Sprague-Dawley rats by administering a single subcutaneous injection of MCT (60 mg/kg, n=12). Rats in the control group are given the vehicle saline (0.5 mL, subcutaneously, n=12). Six rats in each group are given EMD638683 (20 mg/kg) intragastrically once daily starting 2 days prior to MCT treatment. Rats are anesthetized with sodium pentobarbital (50 mg/kg intraperitoneally). Right ventricular systolic pressure (RVSP), right ventricular hypertrophy, and pulmonary vascular remodeling are evaluated 21 days after MCT injection. At the age of 10-12 weeks, male SGK1-/- mice and their wild-type (WT) littermates are given MCT in doses of 60 mg/100 g body weight once a week for 8 consecutive weeks by subcutaneous injection to induce PAH. There are eight mice per group. Mice are anesthetized with sodium pentobarbital (50 mg/kg intraperitoneally) on day 8 after the last MCT administration. Then RVSP, right ventricular hypertrophy, and pulmonary vascular remodeling are evaluated. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.74%

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    EMD638683
    Cat. No.:
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