7-(Methylthio)-2-[(2,2-diphenylacetyl)amino]benzo[1,2-d:4,3-d′]bisthiazole

Description

Gue1654 is a Gβγ-signaling-biased 5-OxoETE receptor antagonist. It inhibits neutrophil and eosinophil shape change and chemotaxis induced by 5-OxoETE (Item No. 34250) but not chemoattractant C5a or prostaglandin D₂ (PGD₂; ). Gue1654 inhibits 5-OxoETE-induced Gβγ-mediated inositol monophosphate (IP₁) production in HEK293 cells transiently expressing the 5-OxoETE receptor, an effect that can be blocked by the Gβγ-inhibitor gallein, but has no effect on IP₁ production induced by stimulation of endogenous Gα_q-linked muscarinic receptors. In a bioluminescence resonance energy transfer (BRET) assay, Gue1654 reduces the 5-OxoETE-induced, but not basal, BRET fluorescence response, indicating disruption of the interaction between ligand-activated 5-OxoETE receptor and Gβγ.

Uses

Gue 1654 is a selective inhibitor of OXE-R Gβγ signaling.