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

SB 216763 

Cat. No.: HY-12012 Purity: 98.01%
Handling Instructions

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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Estimated Time of Arrival: December 31
10 mg USD 84 In-stock
Estimated Time of Arrival: December 31
50 mg USD 252 In-stock
Estimated Time of Arrival: December 31
100 mg USD 432 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 13 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    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.

    SB 216763 purchased from MCE. Usage Cited in: Biochem Pharmacol. 2018 Apr;150:280-292.

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

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

    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 MCE. Usage Cited in: J Cell Biochem. 2018 Jul;119(7):5934-5943.

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

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

    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 MCE. Usage Cited in: J Cell Biochem. 2018 Jul;119(7):5934-5943.

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

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    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

    IC50: 34.3 nM (GSK-3α), 34.3 nM (GSK-3β)[5]

    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].

    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 reverses the ceiling effect because these agents significantly reduce infarct size when the rabbits' hearts are submitted to 30-min CAO[4].

    Molecular Weight

    371.22

    Formula

    C₁₉H₁₂Cl₂N₂O₂

    CAS No.

    280744-09-4

    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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    H2O : < 0.1 mg/mL (insoluble)

    In Vivo:
    • 1.

      SB 216763 is dissolved in DMSO to make stock solutions and then suspended in normal saline[6].

    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
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    SB 216763
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