2. Metabolic Enzyme/Protease
  3. SGK
  4. EMD638683

EMD638683 is a highly selective SGK1 inhibitor, with an IC50 value 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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 264 In-stock
Solution
10 mM * 1 mL in DMSO USD 264 In-stock
Solid
1 mg USD 110 In-stock
5 mg USD 240 In-stock
10 mg USD 380 In-stock
25 mg USD 620 In-stock
50 mg USD 840 In-stock
100 mg USD 1345 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of EMD638683:

EMD638683 Related Antibodies

Top Publications Citing Use of Products

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

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

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

    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 MedChemExpress. Usage Cited in: Environ Toxicol Pharmacol. 2014 Sep;38(2):374-8.  [Abstract]

    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.

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    SGK1 SGK3

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target

    SGK1

     

    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    EMD638683 Related Antibodies
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    364.34

    Formula

    C18H18F2N2O4
    CAS No.
    Appearance

    Solid

    Color

    Off-white to light brown

    SMILES

    CC1=C(CC)C(C(NNC(C(O)C2=CC(F)=CC(F)=C2)=O)=O)=CC=C1O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (137.23 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.89%

    COA (245 KB) RP-HPLC (204 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [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]

    Rats 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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.7447 mL 13.7234 mL 27.4469 mL 68.6172 mL
    5 mM 0.5489 mL 2.7447 mL 5.4894 mL 13.7234 mL
    10 mM 0.2745 mL 1.3723 mL 2.7447 mL 6.8617 mL
    15 mM 0.1830 mL 0.9149 mL 1.8298 mL 4.5745 mL
    20 mM 0.1372 mL 0.6862 mL 1.3723 mL 3.4309 mL
    25 mM 0.1098 mL 0.5489 mL 1.0979 mL 2.7447 mL
    30 mM 0.0915 mL 0.4574 mL 0.9149 mL 2.2872 mL
    40 mM 0.0686 mL 0.3431 mL 0.6862 mL 1.7154 mL
    50 mM 0.0549 mL 0.2745 mL 0.5489 mL 1.3723 mL
    60 mM 0.0457 mL 0.2287 mL 0.4574 mL 1.1436 mL
    80 mM 0.0343 mL 0.1715 mL 0.3431 mL 0.8577 mL
    100 mM 0.0274 mL 0.1372 mL 0.2745 mL 0.6862 mL
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    EMD638683 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    EMD6386831181770-72-8EMD 638683EMD-638683SGKSerum-glucocorticoid regulated kinaseSerum and glucocorticoid-regulated kinaseInhibitorinhibitorinhibit

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