1334294-76-6

1334294-76-6 structure

Name: GSK682753A
Chemical Name: GSK682753A
CAS Number: 1334294-76-6
Molecular Formula: C₂₃H₂₁Cl₃N₂O₃
Molecular Weight: 479.78
Catalog: Signaling Pathways GPCR/G Protein EBI2/GPR183
Create Date: 2018-01-19 20:42:54
Modify Date: 2024-01-10 16:47:00
GSK682753A is a selective and highly potent inverse agonist of the epstein-barr virus-induced receptor 2 (EBI2) with an IC50 of 53.6 nM.

Name	GSK682753A

Description	GSK682753A is a selective and highly potent inverse agonist of the epstein-barr virus-induced receptor 2 (EBI2) with an IC50 of 53.6 nM.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> EBI2/GPR183 Research Areas >> Inflammation/Immunology
Target	IC50: 53.6 nM (EBI2)[1]
In Vitro	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[1].
Cell Assay	The effect of GSK682753A on cAMP-induced CREB activation is measured. GSK682753A at varying concentrations is added when the transfection is stopped with a DMSO concentration after compound addition of 0.1%. The CREB activity is determined 24 h after transfection using the LucLite substrate[1].