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STING agonist diABZI compound 2

Chemical Structure : STING agonist diABZI compound 2

CAS No.: 2138300-40-8

STING agonist diABZI compound 2 (STING agonist diABZI 2)

Catalog No.: PC-35783Not For Human Use, Lab Use Only.

STING agonist diABZI compound 2 is an amidobenzimidazole (ABZI)-based compound that functions as a STING agonist with Kd of 1.6 nM (binding of endogenous full-length STING, THP-1 cell lysates).

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Biological Activity

STING agonist diABZI compound 2 is an amidobenzimidazole (ABZI)-based compound that functions as a STING agonist with Kd of 1.6 nM (binding of endogenous full-length STING, THP-1 cell lysates).
STING agonist diABZI compound 2 caused dose-dependent phosphorylation of IRF3 and STING that was inhibited by the TBK1 inhibitor BX795, induced dose-dependent secretion of IFN-β with EC50 of 3.1 uM in PBMCs (18-fold more potent than cGAMP).
STING agonist diABZI compound 2 promotes production of IFN-γ-induced protein 10 (IP-10), IL-6 and TNFα by a mechanism that is dependent on STING-mediated activation of TBK1.
Unlike cGAMP and DMXAA, compound 2 efficiently activates STING function while maintaining an open STING confirmation.

Physicochemical Properties

M.Wt 678.758
Formula C34H38N12O4
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

1,1'-(butane-1,4-diyl)bis(2-(1-ethyl-3-methyl-1H-pyrazole-5-carboxamido)-1H-benzo[d]imidazole-5-carboxamide)

References

1. Ramanjulu JM, et al. Nature. 2018 Nov 7. doi: 10.1038/s41586-018-0705-y.

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