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STING agonist diABZI compound 3 freebase

Chemical Structure : STING agonist diABZI compound 3 freebase

CAS No.: 2138299-33-7

STING agonist diABZI compound 3 freebase

Catalog No.: PC-35784Not For Human Use, Lab Use Only.

STING agonist diABZI compound 3 is an amidobenzimidazole (ABZI)-based compound that functions as a potent, specific, non-nucleotide STING agonist, induces dose-dependent activation of STING and secretion of IFN-β with EC50 of 130 nM in human PBMCs.

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Biological Activity

STING agonist diABZI compound 3 is an amidobenzimidazole (ABZI)-based compound that functions as a potent, specific, non-nucleotide STING agonist, induces dose-dependent activation of STING and secretion of IFN-β with EC50 of 130 nM in human PBMCs; STING agonist diABZI compound 3 is more than 400-fold more potent than cGAMP, also demonstrates high selectivity against >350 kinases; activates secretion of IFNβ, IL-6, TNF, and KC/GROα (also known as CXCL1) in wild-type but not Sting−/− mice, induces STING-dependent activation of type-I interferon and pro-inflammatory cytokines in vivo via subcutaneous injection; exhibits durable anti-tumour effect and causes complete tumour regression in syngeneic mouse model of colorectal tumours (CT-26) in BALB/c mice.

Physicochemical Properties

M.Wt 849.954
Formula C42H51N13O7
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

(E)-1-(4-(5-Carbamoyl-2-(1-ethyl-3-methyl-1H-pyrazole-5-carboxamido)-7-(3-morpholinopropoxy)-1Hbenzo[d]imidazol-1-yl)but-2-en-1-yl)-2-(1-ethyl-3-methyl-1H-pyrazole-5-carboxamido)-7-methoxy-1Hbenzo[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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