IM-12

Catalog No.S7566

For research use only.

IM-12 is a selective GSK-3β inhibitor with IC50 of 53 nM, and also enhances canonical Wnt signalling.

IM-12 Chemical Structure

CAS No. 1129669-05-1

Selleck's IM-12 has been cited by 12 Publications

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Purity & Quality Control

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Biological Activity

Description IM-12 is a selective GSK-3β inhibitor with IC50 of 53 nM, and also enhances canonical Wnt signalling.
Targets
GSK-3β [1]
(Cell-free assay)
53 nM
In vitro

In hNPCs, IM-12 inhibits GSK-3β activity with IC50 of 3.8 μM and subsequently increases β-catenin concentration significantly. Through the activation of canonical Wnt signalling pathway, IM-12 promotes the neuronal differentiation of human neural progenitor cells. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
ReNcell VM cells  NWDzXXd5WHKxbHnm[ZJifGmxbjDhd5NigQ>? M{jZb|MhfU1? NIiyU4s4OiCq NUXocXplSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDS[W5k\WyuIG\NJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYYSgN{B2VSCjZoTldkA4OiCqcoO= MVOyNFcxQDl|Nx?=
ST14A cells NIDOd5BHfW6ldHnvckBie3OjeR?= NWfBc4o1PiCq MW\Jcohq[mm2aX;uJI9nKEeVSz2zMYJmfGFvbXXkbYF1\WRiV370JJNq\26jbHnu[{BqdiCqdX3hckBUXDF2QTDj[YxteyCjc4Pld5Nm\CCjczDpcoNz\WG|ZTDpckBi[2O3bYXsZZRqd25ib3[gZoV1[S2lYYPlbY4h[XKxdX7kJI52[2yndYOgZYZ1\XJiNjDodpMh[nlibXnjdo9{[2:yaXOgZY5idHm|aYO= NXPEbGZ7OjB5MEi5N|c>

Protocol (from reference)

Kinase Assay:[1]
  • GSK-3β activity assay:

    IC50 of new synthesised compound IM-12 to GSK-3β is determined by a luminometric GSK-3β activity assay. Briefly, compounds are tested in different concentrations diluted in assay buffer 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. Four microlitres of diluted compounds are added to 25 μM pGS-2 peptide substrate, 20 ng recombinant GSK-3β and 1 μM ATP to a total assay volume of 40 μl. The enzymatic reaction is stopped after 30 min of incubation at 30 °C by adding 40 μl KinaseGlo. The luminometric signal is allowed to stabilise for 10 min and the measured with a Glomax® 96 Microplate Luminometer.

Cell Research:[1]
  • Cell lines: ReNcell VM cells
  • Concentrations: 3 μM
  • Incubation Time: 72 hours
  • Method: 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 was determined every 24 h. Cells were exposed to the added drugs during the whole experiment, whereas the media is changed every 24 h.

Solubility (25°C)

In vitro

DMSO 75 mg/mL
(198.72 mM)
Ethanol 10 mg/mL warmed
(26.49 mM)
Water Insoluble

Chemical Information

Molecular Weight 377.41
Formula

C22H20FN3O2

CAS No. 1129669-05-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C2=CC=CC=C2N1)C3=C(C(=O)N(C3=O)C)NCCC4=CC=C(C=C4)F

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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