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LY2090314 GSK-3 inhibitor

Name: LY2090314
Brand: Selleck Chemicals
SKU: S7063
Availability: InStock
Rating: 5 (33 reviews)

Cat.No.S7063

LY2090314 is a potent GSK-3 inhibitor for GSK-3α/β with IC50 of 1.5 nM/0.9 nM; may improve the efficacy of platinum-based chemotherapy regimens. This compound is highly selective towards GSK3 as demonstrated by its fold selectivity relative to a large panel of kinases.

Chemical Structure

Molecular Weight: 512.53

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

Quality Control

Batch: Purity: 99.89%

99.89

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	Activity Description	PMID
human SY5Y cells	Function assay	Inhibition of Glycogen synthase kinase-3 beta dependent Tau protein serine-396 phosphorylation in human SY5Y cells, IC50=0.7 nM	15267232
KB-8-5-11	qHTS assay	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen, Potency = 16.3601 μM.	31515284
KB-3-1	qHTS assay	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	31515284
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	512.53	Formula	C₂₈H₂₅FN₆O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	603288-22-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1CCN(CC1)C(=O)N2CCN3C=C(C4=CC(=CC(=C43)C2)F)C5=C(C(=O)NC5=O)C6=CN=C7N6C=CC=C7

Solubility

In vitro
Batch:

DMSO : 100 mg/mL ( (195.11 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 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.	2.000mg/ml (3.90mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 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.
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.

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] 0.9 nM GSK-3α ^[1] 1.5 nM
In vitro	LY2090314 selectively inhibits the activity of GSK-3 by interrupting ATP binding. This compound is able to stabilize β-catenin. It shows limited efficacy as monotherapy. This chemical enhances the efficacy in solid tumor cancer cell lines in vitro. ^[1]
In vivo	This compound enhances the efficacy in solid tumor cancer xenografts. ^[1]
References	http://meetinglibrary.asco.org/content/82310-102 https://pubmed.ncbi.nlm.nih.gov/25915038/

Applications

Methods	Biomarkers	PMID
Western blot	p-GSK3 / GSK3 / p-AKT Cleaved PARP / Cleaved caspase-3 / Cyclin D1 / Survivin / Mcl-1 LSD1 / Mono-methyl-Histone H3 (K4)	29751783
Immunofluorescence	LSD1	29593255
Growth inhibition assay	Cell viability	29751783

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Frequently Asked Questions

Question 1:
I want to use it in preclinical studies using mice with intracranial xenografts. How could I reconstitute this compound?

Answer:
For in vivo study, DMSO should not be more than 5% because of the toxicity. It can be formulated in hydrochloric acid (0.1 N), and diluted with 0.9% NaCl for animal study according to the reference: http://linkinghub.elsevier.com/retrieve/pii/S0960-9822(06)02671-6 (supplemental Data).

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