LY2090314

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. LY2090314 is highly selective towards GSK3 as demonstrated by its fold selectivity relative to a large panel of kinases.

LY2090314 Chemical Structure

LY2090314 Chemical Structure

CAS: 603288-22-8

Selleck's LY2090314 has been cited by 27 Publications

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Purity & Quality Control

Batch: Purity: 99.89%
99.89

LY2090314 Related Products

Signaling Pathway

Choose Selective GSK-3 Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation 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

Biological Activity

Description 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. LY2090314 is highly selective towards GSK3 as demonstrated by its fold selectivity relative to a large panel of kinases.
Targets
GSK-3β [1] GSK-3α [1]
0.9 nM 1.5 nM
In vitro
In vitro

LY2090314 selectively inhibits the activity of GSK-3 by interrupting ATP binding. LY2090314 is able to stabilize β-catenin. LY2090314 shows limited efficacy as monotherapy. LY3090314 enhances the efficacy of cisplatin and carboplatin in solid tumor cancer cell lines in vitro. [1]

Cell Research Cell lines A375 cells
Concentrations 20 nM
Incubation Time 5 h
Method

Cells were treated with various concentrations of drug for 5 h.

Experimental Result Images Methods Biomarkers Images 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
In Vivo
In vivo

LY2090314 enhances the efficacy of cisplatin and carboplatin in solid tumor cancer xenografts. [1]

Animal Research Animal Models Female athymic nude mice
Dosages 25 mg/kg
Administration i.v

Chemical Information & Solubility

Molecular Weight 512.53 Formula

C28H25FN6O3

CAS No. 603288-22-8 SDF Download LY2090314 SDF
Smiles C1CCN(CC1)C(=O)N2CCN3C=C(C4=CC(=CC(=C43)C2)F)C5=C(C(=O)NC5=O)C6=CN=C7N6C=CC=C7
Storage (From the date of receipt)

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


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In vivo
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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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Frequently Asked Questions

Question 1:
I want to use BI2536 in preclinical studies using mice with intracranial xenografts. How could I reconstitute the compound?

Answer:
For in vivo study, DMSO should not be more than 5% because the toxicity. You can formulated BII2536 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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