1. PI3K/Akt/mTOR Stem Cell/Wnt Autophagy
  2. GSK-3 Autophagy
  3. SB 216763

SB 216763 is potent, selective and ATP-competitive GSK-3 inhibitor with IC50s of 34.3 nM for both GSK-3α and GSK-3β.

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

SB 216763 Chemical Structure

SB 216763 Chemical Structure

CAS No. : 280744-09-4

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Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
5 mg USD 66 In-stock
10 mg USD 92 In-stock
50 mg USD 277 In-stock
100 mg USD 475 In-stock
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Customer Review

Based on 33 publication(s) in Google Scholar

Top Publications Citing Use of Products

27 Publications Citing Use of MCE SB 216763

WB
IF

    SB 216763 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2018 Apr;150:280-292.  [Abstract]

    Expression of c-Myc in MKN-45 cells treated with Lanatoside C and SB216763 at indicated concentrations for 24 h.

    SB 216763 purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2018 Jul;119(7):5934-5943.  [Abstract]

    SB-216763 activates renal autophagy. Representative micrographs showing immunofluorescent staining for LC3-II for among different groups as indicated.

    SB 216763 purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2018 Jul;119(7):5934-5943.  [Abstract]

    SB-216763 activates renal autophagy. Renal protein expression of LC3-I, LC3-II and p62 are assayed in renal tissues treated with Aldo-salt or with Aldo-salt plus SB-216763. SB-216763 increased the Aldo-salt-induced autophagy.

    SB 216763 purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2018 Jul;119(7):5934-5943.  [Abstract]

    SB-216763 activates cardiac autophagy. Images showing immunofluorescent staining for LC3-II for among different groups as indicated.

    SB 216763 purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2018 Jul;119(7):5934-5943.  [Abstract]

    SB-216763 activates cardiac autophagy. Cardiac protein expression of LC3-I, LC3-II, and p62 are assayed in cardiac tissues treated with Aldo-salt or with Aldo-salt plus SB-216763.

    SB 216763 purchased from MedChemExpress. Usage Cited in: Toxicol Appl Pharmacol. 2016 Dec 15;313:195-203.  [Abstract]

    SB 216763 blocks augmentation of phosphor-glycogen synthase and depletion of inhibitory phosphorylated GSK-3β at serine 9 sites, but maintains total GSK-3β levels. Cardiac protection following SB 216763 is dependent on GSK-3β activity inhibition, not on decrease in basal GSK-3β levels. H9c2 cells are treated with 160 nM TP for 24 h after pretreatments with 2 μM SB 216763 or vehicle 2 h later. Levels of p-GS, p-GSK-3β, GSK-3β and GAPDH are measured by western blot.

    View All GSK-3 Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    SB 216763 is potent, selective and ATP-competitive GSK-3 inhibitor with IC50s of 34.3 nM for both GSK-3α and GSK-3β.

    IC50 & Target[5]

    GSK-3α

    34.3 nM (IC50)

    GSK-3β

    34.3 nM (IC50)

    In Vitro

    SB-216763 (10-20 μM) induces β-catenin mediated-transcription in a dose-dependent manner in HEK293 cells. SB-216763 (10, 15 and 20 μM) can maintain mESCs with a pluripotent-like morphology in long-term culture. SB-216763 (10 μM) can maintain J1 mESCs in a pluripotent state for more than a month[2].
    SB-216763 inhibits GSK-3 with IC50 of 34 nM[3].
    SB-216763 is equally effective at inhibiting human GSK-3α and GSK-3β[5].

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

    In Vivo

    SB216763 (20 mg/kg, i.v.) significantly improves the survival of BLM-treated mice. Mice randomized to receive BLM plus SB216763 shows a noteworthy reduction, compared with BLM-treated mice. SB216763 (20 mg/kg, i.v.) reduces the magnitude of BLM-induced alveolitis[1]. SB 216763 (0.2 mg/kg, i.v.) with either 17β-E100 or Geni100 significantly reduce infarct size when the rabbits' hearts are submitted to 30-min CAO[4].

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

    Molecular Weight

    371.22

    Formula

    C19H12Cl2N2O2

    CAS No.
    Appearance

    Solid

    Color

    Orange to red

    SMILES

    O=C(NC1=O)C(C2=CC=C(C=C2Cl)Cl)=C1C3=CN(C4=C3C=CC=C4)C

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (269.38 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.6938 mL 13.4691 mL 26.9382 mL
    5 mM 0.5388 mL 2.6938 mL 5.3876 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, 1 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

    • 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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    Molecular Weight *

    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)

    V1

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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 (6.73 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 (6.73 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      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: 99.82%

    References
    Cell Assay
    [2]

    MESCs maintained with LIF or 10 µM SB-216763 for more than a month are resuspended at 40,000 cells/mL in LIF-free mESC medium. EBs are prepared by a hanging drop procedure. Briefly, 20 µL drops containing mESCs are pipetted on the inside of a 10-cm Petri dish lid. The lids are placed onto Petri dishes containing 10 mL of HBSS and the EBs are allowed to form and grow for 4 days in the incubator. After 4 days, 15-20 EBs are transferred to a well containing LIF-free mESC medium in a 24-well plate. The medium is exchanged every two days and autonomously beating cell aggregates are observed and counted.

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

    Animal Administration
    [1]

    Mice are allocated to four groups (n=12/group) as follows: 1) intratracheal saline + vehicle (25% dimethyl sulfoxide, 25% polyethylene glycol, and 50% saline), 2) intratracheal saline + SB216763 (20 mg/kg) dissolved in vehicle, 3) intratracheal BLM (3 U/kg) + vehicle, and 4) intratracheal BLM + SB216763 (20 mg/kg) in vehicle. Another set of experiments to assess cytokine expression by reverse transcription-PCR is conducted in the mice (n=12/group) to receive 1) intratracheal saline + vehicle, 2) intratracheal BLM, and 3) intratracheal BLM + SB216763. To induce pulmonary fibrosis, BLM is intratracheally administered in mice (n=15/group) on day 0. BLM and saline-treated mice are administered with SB216763 dissolved in vehicle or vehicle alone intravenously at day 0 and then intraperitoneally twice a week until day 28. Mice are sacrificed by CO2 inhalation on days 2, 7, and 28. In the terminal deoxynucleotidyl transferase dUTP nick-end labeling (TUNEL) experiments, the cohorts of mice are as follows: saline-treated (n=6), BLM-treated (n=6), and BLM + SB216763-treated (n=6).

    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, 1 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.6938 mL 13.4691 mL 26.9382 mL 67.3455 mL
    5 mM 0.5388 mL 2.6938 mL 5.3876 mL 13.4691 mL
    10 mM 0.2694 mL 1.3469 mL 2.6938 mL 6.7346 mL
    15 mM 0.1796 mL 0.8979 mL 1.7959 mL 4.4897 mL
    20 mM 0.1347 mL 0.6735 mL 1.3469 mL 3.3673 mL
    25 mM 0.1078 mL 0.5388 mL 1.0775 mL 2.6938 mL
    30 mM 0.0898 mL 0.4490 mL 0.8979 mL 2.2449 mL
    40 mM 0.0673 mL 0.3367 mL 0.6735 mL 1.6836 mL
    50 mM 0.0539 mL 0.2694 mL 0.5388 mL 1.3469 mL
    60 mM 0.0449 mL 0.2245 mL 0.4490 mL 1.1224 mL
    80 mM 0.0337 mL 0.1684 mL 0.3367 mL 0.8418 mL
    100 mM 0.0269 mL 0.1347 mL 0.2694 mL 0.6735 mL
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    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.

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