A membrane-permeant amidobenzobisthiazolo compound that modulates OXE-R-G_βγ coupling upon receptor stimulation via direct OXE-R interaction, but not preexisting OXE-R-G_αβ interaction. Shown to selectively inhibit OXE-R-G_βγ coupling-mediated, but not OXE-R-G_α-mediated, downstream signalings in HEK293 as well as primary human eosinophils and neutrophils (Effective Conc. 1 to 30 μM), displaying no inhibitory activity against cellular functions mediated by G_α or G_βγ when coupled to other GPCRs, including PGD₂ receptor CRTH2 (DP2), IL8 receptors CXCR1/2, muscarinic receptor, and C5a receptor. Comparing to Gallein (Cat. No. 371708), Gue1654 does not exert its activity via direct G_βγ interaction.

A membrane-permeant amidobenzobisthiazolo compound that modulates OXE-R-G_βγ coupling upon receptor stimulation via direct OXE-R interaction, without affecting preexisting OXE-R-G_αβ interaction. Selectively inhibits OXE-R-G_βγ coupling-mediated, but not OXE-R-G_α-mediated, downstream cellular signalings (Effective Conc. 1 to 30 μM), displaying no inhibitory activity against cellular functions mediated by G_α or G_βγ when coupled to other GPCRs. Comparing to Gallein (Cat. No. 371708), Gue1654 does not exert its activity via direct G_βγ interaction.

OXE-R-G_βγ coupling

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

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