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IM-12 GSK-3 inhibitor

Cat.No.S7566

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

Chemical Structure

Molecular Weight: 377.41

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.01%

99.01

Related Targets	PI3K Akt mTOR AMPK ATM/ATR DNA-PK PDPK1 PTEN PP2A PDK PI4K PIKfyve MELK
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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description
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
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
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	377.41	Formula	C₂₂H₂₀FN₃O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1129669-05-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=C(C2=CC=CC=C2N1)C3=C(C(=O)N(C3=O)C)NCCC4=CC=C(C=C4)F

Solubility

In vitro
Batch:

DMSO : 75 mg/mL (198.72 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.750mg/ml (9.94mM)	Taking the 1 mL working solution as an example, add 50 μL of 75 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.625mg/ml (1.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 12.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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.

Mechanism of Action

Targets/IC₅₀/Ki	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, this compound promotes the neuronal differentiation of human neural progenitor cells. ^[1]
Kinase Assay	GSK-3β activity assay
Kinase Assay	IC50 of new synthesised compound IM-12 to GSK-3β is determined by a luminometric GSK-3β activity assay. Briefly, this compound is 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/20708937/

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