DC Chemicals · Product datasheet

GSK682753A — Datasheet

CAT. NO. DC10391

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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.

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