GSK682753A chemical structure
Chemical structureResearch use only
CAT. NO. DC10391Featured

GSK682753A

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Product overview

Description & Application

GSK682753 is a selective and highly potent inverse agonist for murine as well as human EBI2 with inhibition of G protein-dependent signals as well as signals that are probably G protein-independent. In cAMP-response element-binding protein-based reporter and guanosine5'-3-O-(thio)-triphosphate (GTPγS) binding assays, the potency of this compound is 2.6-53.6 nM, and its inhibitory efficacy is 75%. GSK682753A dose-dependently inhibits EBI2 with an IC50of 53.6 nM. GSK682753A inhibits ERK phosphorylation, GTPγS binding, and cAMP-response element-binding protein activation with similar potency.

ParameterValue
Chemical NameGSK682753A
CAS No.1334294-76-6
SynonymsGSK682753A;GSK-682753A;8-[(E)-3-(4-Chlorophenyl)prop-2-enoyl]-3-[(3,4-dichlorophenyl)methyl]-1-oxa-3,8-diazaspiro[4.5]decan-2-one;EBI2 inhibitor GS682753A;F85517;(E)-8-(3-(4-Chlorophenyl)acryloyl)-3-(3,4-dichlorobenzyl)-1-oxa-3,8-diazaspiro[4.5]decan-2-one;GTPL13053;AKOS030260724;GLXC-03695;DA-53755;HY-101192;CS-6260;1334294-76-6;Z2941211650;8-[(2E)-3-(4-Chlorophenyl)-1-oxo-2-propen-1-yl]-3-[(3,4-dichlorophenyl)methyl]-1-oxa-3,8-diazaspiro[4.5]decan-2-one;MS-28924
FormulaC23H21Cl3N2O3
M.Wt479.7834
SMILESClC1=C(C([H])=C([H])C(=C1[H])C([H])([H])N1C(=O)OC2(C1([H])[H])C([H])([H])C([H])([H])N(C(/C(/[H])=C(\[H])/C1C([H])=C([H])C(=C([H])C=1[H])Cl)=O)C([H])([H])C2([H])[H])Cl
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

GSK682753 is a selective and highly potent inverse agonist for murine as well as human EBI2 with inhibition of G protein-dependent signals as well as signals that are probably G protein-independent. In cAMP-response element-binding protein-based reporter and guanosine5'-3-O-(thio)-triphosphate (GTPγS) binding assays, the potency of this compound is 2.6-53.6 nM, and its inhibitory efficacy is 75%. GSK682753A dose-dependently inhibits EBI2 with an IC50of 53.6 nM. GSK682753A inhibits ERK phosphorylation, GTPγS binding, and cAMP-response element-binding protein activation with similar potency.

In Vitro

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In Vivo

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References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

Product documentation

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Handling guide

2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Solution calculator

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