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Gue-1654

Chemical Structure : Gue-1654

CAS No.: 397290-30-1

Gue-1654 (Gue 1654;Gue1654)

Catalog No.: PC-70005Not For Human Use, Lab Use Only.

Gue-1654 (GUE 1654) is a small-molecule that inhibits Gβγ but not Gα signaling triggered upon activation of Gα(i)-βγ by the chemoattractant receptor OXE-R (Oxoeicosanoid receptor) in both recombinant and human primary cells.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Gue-1654 (GUE 1654) is a small-molecule that inhibits Gβγ but not Gα signaling triggered upon activation of Gα(i)-βγ by the chemoattractant receptor OXE-R (Oxoeicosanoid receptor) in both recombinant and human primary cells.
Gue-1654 blocks β-arrestin2 recruitment in HEK293 cells overexpressing OXE-R and ERK1/2 phosphorylation in human eosinophils and neutrophils.
Gue-1654 is the first small-molecule inhibitor for the oxoeicosanoid receptor (OXE-R) and the first probe to uncouple Gα and Gβγ signaling within a heterotrimer for any GPCR.

Physicochemical Properties

M.Wt 447.589
Formula C23H17N3OS3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(7-(methylthio)benzo[1,2-d:4,3-d']bis(thiazole)-2-yl)-2,2-diphenylacetamide

References

1. Blättermann S, et al. Nat Chem Biol. 2012 Jul;8(7):631-8.

2. Konya V, et al. J Immunol. 2014 May 15;192(10):4774-82.

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