LY2090314

Catalog No.S7063

For research use only.

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

CAS No. 603288-22-8

Selleck's LY2090314 has been cited by 26 publications

Purity & Quality Control

Choose Selective GSK-3 Inhibitors

Other GSK-3 Products

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

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human SY5Y cells MXLGeY5kfGmxbjDhd5NigQ>? NUX0PVdUUW6qaXLpeIlwdiCxZjDHcJlkd2enbjDzfY51cGG|ZTDrbY5ie2VvMzDi[ZRiKGSncHXu[IVvfCCWYYWgdJJwfGWrbjDz[ZJqdmVvM{m2JJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDTXVV[KGOnbHzzMEBKSzVyPUCuO{BvVQ>? MnrWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTV{NkeyN|IoRjF3Mk[3NlMzRC:jPh?=
KB-8-5-11 NXK0ZXdYeUiWUzDhd5NigQ>? Mn7BVE1odHmlb4Dyc5RmcW5ic4Xid5Rz[XSnczDp[IVvfGmoaXXkJIlvKEuELUitOU0yOSCjZHXuc4NiemOrbn;tZUBk\WyuIHzpcoUtKHGKVGOgeIhmemGyZYX0bYMhdGmkcnHyfUB{[3KnZX6sJHBwfGWwY4mgQUAyPi5|NkCxJO69VS5? M3\0[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNUG1Nlg1Lz5|MUWxOVI5PDxxYU6=
KB-3-1 MkLrdWhVWyCjc4PhfS=> NXrTbYwzWC2pbInjc5Bzd3SnaX6gd5Vje3S{YYTld{Bq\GWwdHnmbYVlKGmwIFvCMVMuOSCjZHXuc4NiemOrbn;tZUBk\WyuIHzpcoUtKHGKVGOgeIhmemGyZYX0bYMhdGmkcnHyfUB{[3KnZX6= NI\4d5k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUWxOVI5PCd-M{G1NVUzQDR:L3G+
Assay
Methods Test Index 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 29593255
Immunofluorescence LSD1 29593255
Growth inhibition assay Cell viability 29751783
In vivo

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

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(195.11 mM)
Ethanol 2 mg/mL warmed
(3.9 mM)
Water Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+45% PEG 300+ddH2O
For best results, use promptly after mixing.

17mg/mL

Chemical Information

Molecular Weight 512.53
Formula

C28H25FN6O3

CAS No. 603288-22-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CCN(CC1)C(=O)N2CCN3C=C(C4=CC(=CC(=C43)C2)F)C5=C(C(=O)NC5=O)C6=CN=C7N6C=CC=C7

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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 %

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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

Mass Concentration Volume Molecular Weight

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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