An EBI2 inverse agonist
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GSK682753A

Item No. 45381

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
8-[(2E)-3-(4-chlorophenyl)-1-oxo-2-propen-1-yl]-3-[(34-,dichlorophenyl)methyl]-1-oxa-3,8-diazaspiro[4.5]decan-2-one
CAS Number
1334294-76-6
Molecular Formula
C23H21Cl3N2O3
Formula Weight
479.8
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Methanol: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C1OC2(CCN(CC2)C(/C=C/C3=CC=C(C=C3)Cl)=O)CN1CC4=CC(Cl)=C(C=C4)Cl
InChi Code
InChI=1S/C23H21Cl3N2O3/c24-18-5-1-16(2-6-18)4-8-21(29)27-11-9-23(10-12-27)15-28(22(30)31-23)14-17-3-7-19(25)20(26)13-17/h1-8,13H,9-12,14-15H2/b8-4+
InChi Key
RDDLWMWIRXGSJM-XBXARRHUSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

    $135

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    10 mg

    $216

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    25 mg

    $473

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    Product Description

    GSK682753A is an Epstein-Barr virus-induced G protein-coupled receptor 2 (EBI2) inverse agonist.1 It inhibits CREB activity in a reporter assay using HEK293 cells transiently transfected with EBI2 and Gqi4myr, a chimeric Gα subunit that recognizes Gαi receptors but activates Gαq-mediated pathways (IC50 = 53.6 nM). GSK682753A (0.001-1 µM) inhibits antibody-induced proliferation of B cells isolated from transgenic mice overexpressing human EBI2.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Benned-Jensen, T., Smethurst, C., Holst, P.J., et al. Ligand modulation of the Epstein-Barr virus-induced seven-transmembrane receptor EBI2: Identification of a potent and efficacious inverse agonist. The Journal of Biological Chemisty 286(33), 29292-29302 (2011).