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IM-12 (Synonyms: GSK3β Inhibitor XIX)

Catalog No.GC16617

GSK-3β inhibitor, potent

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IM-12 Chemical Structure

Cas No.: 1129669-05-1

Size Price Stock Qty
10mM (in 1mL DMSO)
$61.00
In stock
10mg
$53.00
In stock
50mg
$186.00
In stock
200mg
$400.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Kinase experiment:

Cells are lysed in RIPA buffer, supplemented with protease and phosphatase inhibitors and centrifuged for 5 min at 15,000 rpm. Immunoprecipitation of GSK-3β is performed with a specific mouse monoclonal anti GSK-3β [G8] antibody with 5 μg/sample for 2 h at 4°C. The bound protein is precipitated with Protein A/G-Plus agarose-beads (10 μL beads per sample). GSK-3β kinase activity is measured in a reaction mixture containing final concentrations of: 4 mM MOPS pH 7.2; 0.4 mM EDTA; 1 mM EGTA; 2.5 mM β-glycerophosphate; 4 mM MgCl2; 40 μM BSA; 0.05 mM DTT. 10 μg/sample pGS-2 peptide substrate is used[1].

Cell experiment:

To measure viable cells, 50-100 μL of cell suspension is analyzed using CASY technology with the appropriate program. ReNcell VM cells are seeded at a defined cell number and proliferated for 24 h. Then the medium is changed to proliferation medium with added substances at indicated concentrations. The cell number is determined every 24 h. Cells are exposed to the added drugs during the whole experiment, whereas the media is changed every 24 h[1].

References:

[1]. Schmole AC, et al. Novel indolylmaleimide acts as GSK-3beta inhibitor in human neural progenitor cells. Bioorg Med Chem. 2010 Sep 15;18(18):6785-95.

Background

IM-12 is a potent inhibitor of GSK-3β with IC50 value of 53 nM [1].

Glycogen synthase kinase-3β (GSK-3β) is a proline-directed serine-threonine kinase and is involved in neuronal cell development, energy metabolism and body pattern formation. Inhibition of GSK-3β can cause β-catenin accumulation.

IM-12 is a potent GSK-3β inhibitor. In ReNcell VM cells, IM-12 significantly increased total β-catenin by 27% and at a concentration of 3 µM increased the β-catenin amount most. In ReNcell VM cells, IM-12 (3 µM) inhibited GSK-3β to a remaining activity of 27 ± 5%. Also, IM-12 significantly increased the cell doubling time to 26.5 ± 0.9 h and significantly inhibited cell proliferation. In ST14A cells, IM-12 caused an accumulation of β-catenin around the nucleus. In ReNcell VM cells transfected with TOPFlash, IM-12 increased TCF-activity. In cells transfected with TOP and pCAGGS-S33Y (a vector containing β-catenin), IM-12 significantly increased TCF-activity by 270%. In ReNcell VM cells, IM-12 significantly increased the level of βIIItub+ cells to 3.7 ± 0.7%, which suggested that IM-12 increased neuronal differentiation [1].

Reference:
[1].  Schmöle AC, Brennführer A, Karapetyan G, et al. Novel indolylmaleimide acts as GSK-3beta inhibitor in human neural progenitor cells. Bioorg Med Chem, 2010, 18(18): 6785-6795.

Chemical Properties

Cas No. 1129669-05-1 SDF
Synonyms GSK3β Inhibitor XIX
Canonical SMILES FC1=CC=C(C=C1)CCNC2=C(C(N(C)C2=O)=O)C3=C(C)NC4=CC=CC=C34
Formula C22H20FN3O2 M.Wt 377.41
Solubility ≥ 18.85mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.6496 mL 13.2482 mL 26.4964 mL
5 mM 0.5299 mL 2.6496 mL 5.2993 mL
10 mM 0.265 mL 1.3248 mL 2.6496 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Average Rating: 5 ★★★★★ (Based on Reviews and 37 reference(s) in Google Scholar.)

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