GSK682753A_product_DataBase

Bioactivity	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.
Target	IC50: 53.6 nM (EBI2)
Invitro	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].
Name	GSK682753A
CAS	1334294-76-6
Formula	C23H21Cl3N2O3
Molar Mass	479.78
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Reference	[1]. Benned-Jensen T, et al. Ligand modulation of the Epstein-Barr virus-induced seven-transmembrane receptor EBI2: identification of a potent and efficacious inverse agonist. J Biol Chem. 2011 Aug 19;286(33):29292-302.

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