2. Metabolic Enzyme/Protease Immunology/Inflammation Apoptosis
  3. SGK NOD-like Receptor (NLR) Interleukin Related Apoptosis
  4. EMD638683

EMD638683 is an orally active SGK1 inhibitor with an IC50 of 3 μM. EMD638683 exhibits strong inhibition against SGK1, moderate inhibition against SGK2 and SGK3, and shows excellent selectivity for other AGC kinase family members. EMD638683 has antihypertensive activity by inhibiting SGK1, and independently of the blood pressure-lowering effect, it effectively prevents heart inflammation and fibrosis caused by hypertension by inhibiting the cardiac NLRP3 inflammation body/ IL-1β axis. EMD638683 promotes apoptosis of colon cancer cells and sensitizes radiotherapy. EMD638683 (S-Form) can be used in research related to hypertension, hypertensive heart damage, and colon cancer.

For research use only. We do not sell to patients.

CAS No. : 1181770-72-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 18 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.

    View All SGK Isoform Specific Products:

    View All Isoforms
    SGK1 SGK3 SGK2

    View All NOD-like Receptor (NLR) Isoform Specific Products:

    View All Isoforms
    NLRP3 NLRP1 NOD1 NOD2

    View All Interleukin Related Isoform Specific Products:

    View All Isoforms
    IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    EMD638683 is an orally active SGK1 inhibitor with an IC50 of 3 μM. EMD638683 exhibits strong inhibition against SGK1, moderate inhibition against SGK2 and SGK3, and shows excellent selectivity for other AGC kinase family members. EMD638683 has antihypertensive activity by inhibiting SGK1, and independently of the blood pressure-lowering effect, it effectively prevents heart inflammation and fibrosis caused by hypertension by inhibiting the cardiac NLRP3 inflammation body/ IL-1β axis. EMD638683 promotes apoptosis of colon cancer cells and sensitizes radiotherapy. EMD638683 (S-Form) can be used in research related to hypertension, hypertensive heart damage, and colon cancer[1][2][3].

    IC50 & Target[3]

    SGK1

    3 μM (IC50)

    In Vitro

    EMD638683 (50 μM; 9-25 h) inhibits NLRP3 inflammasome activation and IL-1β secretion in mouse bone marrow-derived macrophages induced by angiotensin II (Ang II) by targeting NLRP3 expression[2].
    EMD638683 (50 μM; 25-49 h) inhibits angiotensin II-induced transformation of primary mouse cardiac fibroblasts into myofibroblasts by reducing IL-1β secretion from macrophages[2].
    EMD638683 (50 μM; 96 h) enhances radiation-induced apoptotic death of Caco-2 colon cancer cells[3].

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

    EMD638683 Related Antibodies

    Apoptosis Analysis[3]

    Cell Line: Caco-2 cells
    Concentration: 50 μM
    Incubation Time: 24 h pre-incubation, 72 h post-radiation incubation
    Result: Enhanced radiation-induced apoptotic cell death in Caco-2 colon carcinoma cells, including augmented cell shrinkage, mitochondrial depolarization, caspase 3 activation, phosphatidylserine exposure, and late apoptosis.
    In Vivo

    EMD638683 (600 mg/kg, administered via mixed diet for 4 consecutive days) normalizes systolic blood pressure in hyperinsulinemic, salt-loaded wild-type mice, reducing their blood pressure from 111 mmHg to 87 mmHg over the 4-day treatment period[1].
    EMD638683 (600 mg/kg, administered via mixed feed for 4 weeks) prevents hypertension in wild-type mice treated with 10% fructose in isotonic saline for 4 weeks[1].

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

    Animal Model: SV129 original background backcrossed 4 generations to C57BL/6J sgk1+/+ wild type (mixed gender, 4 months old, hyperinsulinemic salt-loaded)[1]
    Dosage: 600 mg/kg
    Administration: p.o.; continuous in chow; 4 days
    Result: Normalized systolic blood pressure from 111 mmHg to 87 mmHg.
    Significantly increased urinary flow rate.
    Significantly decreased body weight.
    Caused no significant changes to fluid intake, food intake, or urinary Na+ and K+ excretion.
    Increased blood pressure to 106 mmHg after returning to placebo food.
    Animal Model: SV129 original background backcrossed 4 generations to C57BL/6J sgk1+/+ wild type (mixed gender, 7 to 10 months old, fructose/salt-induced hypertension)[1]
    Dosage: 600 mg/kg
    Administration: p.o.; continuous in chow; 4 weeks
    Result: Prevented the fructose/salt-induced rise in systolic blood pressure.
    Resulted in significantly lower systolic blood pressure compared to placebo-treated mice.
    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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    Volume (start)

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    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: 99.94%

    SDS (396 KB)

    COA (245 KB) RP-HPLC (244 KB)

    Handling Instructions (2659 KB)
    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-638683SGKNOD-like Receptor (NLR)Interleukin RelatedApoptosisSerum-glucocorticoid regulated kinaseSerum and glucocorticoid-regulated kinaseILInhibitorinhibitorinhibit

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