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GSK682753A

Catalog No. T11498 CAS 1334294-76-6

GSK682753A is a selective and highly potent inverse agonist of the epstein-barr virus-induced receptor 2 (EBI2; IC50: 53.6 nM).

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GSK682753A, CAS 1334294-76-6

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2 mg	5 days	$ 95.00

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Biological Description

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Description	GSK682753A is a selective and highly potent inverse agonist of the epstein-barr virus-induced receptor 2 (EBI2; IC50: 53.6 nM).
Targets&IC50	EBI2/GPR183:53.6 nM
In vitro	GSK682753A exhibits dose-dependent inhibition of EBI2, achieving an IC50 of 53.6 nM. It demonstrates similar potency in inhibiting ERK phosphorylation, GTPγS binding, and activation of the cAMP-response element-binding protein (CREB). Additionally, GSK682753A acts as a selective and highly potent inverse agonist for both murine and human EBI2, effectively blocking G protein-dependent and potentially G protein-independent signals. In assays using cAMP-response element-binding protein-based reporters and guanosine 5'-3-O-(thio)-triphosphate (GTPγS) binding, GSK682753A shows a potency range of 2.6-53.6 nM and achieves an inhibitory efficacy of 75%.

Molecular Weight	479.78
Formula	C23H21Cl3N2O3
CAS No.	1334294-76-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 27 mg/mL (56.28 mM)

References and Literature

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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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

GSK682753A 1334294-76-6 Others GSK-682753A inhibitor inhibit

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