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

SB 216763 

Cat. No.: HY-12012 Purity: 97.00%
Data Sheet SDS Handling Instructions

SB 216763 is potent and selective glycogen synthase kinase-3 (GSK-3) inhibitor, with IC50 value of 34 nM.

For research use only. We do not sell to patients.
SB 216763 Chemical Structure

SB 216763 Chemical Structure

CAS No. : 280744-09-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO $55 In-stock
5 mg $50 In-stock
10 mg $70 In-stock
50 mg $210 In-stock
100 mg $360 In-stock
200 mg   Get quote  
500 mg   Get quote  

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    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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    SB 216763 is potent and selective glycogen synthase kinase-3 (GSK-3) inhibitor, with IC50 value of 34 nM.

    IC50 & Target

    IC50: 34 nM (GSK-3)[3]

    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].

    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].

    References
    Preparing Stock Solutions
    Concentration Volume 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
    10 mM 0.2694 mL 1.3469 mL 2.6938 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [2]

    SB-216763 is dissolved in 0.1% DMSO.

    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]

    SB 216763 is dissolved in vehicle (25% dimethyl sulfoxide, 25% polyethylene glycol, and 50% saline).

    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
    Molecular Weight

    371.22

    Formula

    C₁₉H₁₂Cl₂N₂O₂

    CAS No.

    280744-09-4

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    SB 216763 is dissolved in DMSO to make stock solutions and then suspended in normal saline[5].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

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    Inquiry Information

    Product Name:
    SB 216763
    Cat. No.:
    HY-12012
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