IM-12

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

IM-12 Chemical Structure

IM-12 Chemical Structure

CAS No. 1129669-05-1

Purity & Quality Control

IM-12 Related Products

Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
ReNcell VM cells  Proliferation assay 3 uM 72 h Antiproliferative activity against human ReNcell VM cells assessed as reduction of cell proliferation at 3 uM after 72 hrs 20708937
ST14A cells Function assay 6 h Inhibition of GSK-3-beta-mediated Wnt signaling in human ST14A cells assessed as increase in accumulation of beta-casein around nucleus after 6 hrs by microscopic analysis 20708937
Click to View More Cell Line Experimental Data

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 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]
Kinase Assay 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 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.

Chemical Information & Solubility

Molecular Weight 377.41 Formula

C22H20FN3O2

CAS No. 1129669-05-1 SDF Download IM-12 SDF
Smiles CC1=C(C2=CC=CC=C2N1)C3=C(C(=O)N(C3=O)C)NCCC4=CC=C(C=C4)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 75 mg/mL ( (198.72 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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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