2. MAPK/ERK Pathway Autophagy
  3. p38 MAPK Autophagy
  4. SB 239063

SB 239063 is a potent, selective and orally active p38 MAPK inhibitor, exhibits an IC50 of 44 nM for recombinant purified human p38α, with equipotent inhibitory activity against p38α and p38β. SB 239063 has no effect on p38γ or p38δ. With anti-asthma activity and also be used to enhance memory which is impaired due to aging or medical conditions, such as, AD.

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

SB 239063 Chemical Structure

SB 239063 Chemical Structure

CAS No. : 193551-21-2

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 89 In-stock
Solution
10 mM * 1 mL in DMSO USD 89 In-stock
Solid
1 mg USD 55 In-stock
5 mg USD 110 In-stock
10 mg USD 198 In-stock
25 mg USD 429 In-stock
50 mg USD 770 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 30 publication(s) in Google Scholar

SB 239063 Related Antibodies

Top Publications Citing Use of Products

    SB 239063 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Jun 28;37(1):128.  [Abstract]

    MHCC-97H cells are transfected with control or supervillin-specific siRNA for 48 h, exposed to hypoxia for 16 h, and lysates are assayed for the relative amounts of GTP-loaded (activated) Rac1, Cdc42, and RhoA. Cells that have been transfected with control RNAi are treated with a PD0325901 or SB239063 before assaying for GTP-Rac1, Cdc42, and RhoA levels.

    SB 239063 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2017 Nov 14;8:808.  [Abstract]

    Immunofluorescence staining of α-actinin and the cell surface area of cardiomyocytes in the indicated groups (n=5 samples and n=100+cells per group).

    SB 239063 purchased from MedChemExpress. Usage Cited in: China Biotechnology. 2017, 37(12): 40-48.

    The Western blot analysis of HOG1 and Phospho-HOG1.

    SB 239063 purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2016 Sep;38:54-60.  [Abstract]

    The protective role of p38 MAPK inhibition in II/R-induced ALI and regulation of AQP4 in rats. HE staining and Lung wet/dry weight ratio show obvious evidences of ALI and lung edema. Western blot and immunofluorescent staining confirm the increased expression levels of AQP4 and P-p38 MAPK protein in the lung tissues. Then, the p38 MAPK inhibitor is administrated intraperitoneally. Results show that p38 MAPK inhibition downregulates AQP4 expression in the lungs and protected lung from acute injur

    View All p38 MAPK Isoform Specific Products:

    View All Isoforms
    p38 MAPK p38α p38β MAPK13 p38δ p38γ

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    SB 239063 is a potent, selective and orally active p38 MAPK inhibitor, exhibits an IC50 of 44 nM for recombinant purified human p38α, with equipotent inhibitory activity against p38α and p38β. SB 239063 has no effect on p38γ or p38δ. With anti-asthma activity and also be used to enhance memory which is impaired due to aging or medical conditions, such as, AD[1][2].

    IC50 & Target

    IC50: 44 nM (Human p38α)[1]
    In Vitro

    SB 239063 (0.1–10 μM ; 29 hours, 47 hours) increases apoptosis of eosinophils in a dose-related in the presence of 10 pM IL-5 at every time point from 21 hours onwards[1].
    SB 239063 potently inhibits IL-1 and TNF- a production in LPS-stimulated human peripheral blood monocytes with IC50 values of 120 nM and 350 nM, respectively[1].

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

    SB 239063 Related Antibodies

    Apoptosis Analysis[1]

    Cell Line: Eosinophils (guinea pig BALs)
    Concentration: 0.1μM, 1μM, 10μM
    Incubation Time: 29 hours, 47 hours
    Result: Increased apoptosis of eosinophils in a dose-related in the presence of 10 pM IL-5 at every time point from 21 hours onwards.
    In Vivo

    SB 239063 (12 mg/kg; p.o.; 1 hour before and 4 hours after OA challenge; b.i.d. for 3 days) significantly inhibits the resultant antigen-induced airway eosinophilia[1].
    SB 239063 (12 mg/kg; p.o.) almost abolishes ovalbumin (OA)-induced airway eosinophilia (~ 93% inhibition) by inhalation[1].
    SB 239063 is a potent inhibitor of LPS-induced TNF-alpha production in the mouse peritoneal cavity with an EC50 of 5.8 mg/kg (2.8–10.3; 95% CL)[1].

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

    Animal Model: Male BALB/c mice (18–20 g)[1]
    Dosage: 12 mg/kg
    Administration: Oral administration; 1 h before and 4 h after OA challenge; bis in die for 3 days
    Result: Significantly inhibited the resultant antigen-induced airway eosinophilia.
    Molecular Weight

    368.40

    Formula

    C20H21FN4O2
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    COC1=NC=CC(C2=C(N=CN2[C@H]3CC[C@H](O)CC3)C4=CC=C(F)C=C4)=N1
    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 : 33.33 mg/mL (90.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7144 mL 13.5722 mL 27.1444 mL
    5 mM 0.5429 mL 2.7144 mL 5.4289 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
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    Volume
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

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    C2

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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 (6.79 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (6.79 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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    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: 99.61%

    COA (254 KB) LCMS (95 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 2.7144 mL 13.5722 mL 27.1444 mL 67.8610 mL
    5 mM 0.5429 mL 2.7144 mL 5.4289 mL 13.5722 mL
    10 mM 0.2714 mL 1.3572 mL 2.7144 mL 6.7861 mL
    15 mM 0.1810 mL 0.9048 mL 1.8096 mL 4.5241 mL
    20 mM 0.1357 mL 0.6786 mL 1.3572 mL 3.3931 mL
    25 mM 0.1086 mL 0.5429 mL 1.0858 mL 2.7144 mL
    30 mM 0.0905 mL 0.4524 mL 0.9048 mL 2.2620 mL
    40 mM 0.0679 mL 0.3393 mL 0.6786 mL 1.6965 mL
    50 mM 0.0543 mL 0.2714 mL 0.5429 mL 1.3572 mL
    60 mM 0.0452 mL 0.2262 mL 0.4524 mL 1.1310 mL
    80 mM 0.0339 mL 0.1697 mL 0.3393 mL 0.8483 mL
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    SB 239063 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:

    SB 239063193551-21-2SB239063SB-239063p38 MAPKAutophagyInhibitorinhibitorinhibit

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