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STING activator Compound 53

Chemical Structure : STING activator Compound 53

CAS No.: 2259624-71-8

STING activator Compound 53 (STING agonist C53)

Catalog No.: PC-73368Not For Human Use, Lab Use Only.

STING activator Compound 53 is a potent small molecule activator of human STING with functional EC50 of 183 nM in immortalised and primary cells.

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Purity & Documentation Purity: 98.46% (HPLC) Select Batch:

Biological Activity

STING activator Compound 53 is a potent small molecule activator of human STING with functional EC50 of 183 nM in immortalised and primary cells.
Compound 53 directly activates STING from across the major protein variants found in the human population and from both recombinant and primary cells.
Compound 53 induces a broad panel of cytokines and markers of dendritic cell maturation consistent with its activation of STING.
Compound 53 binds to a cryptic pocket in the STING transmembrane domain, between the two subunits of the STING dimer. promotes the oligomerization and activation of human STING through a mechanism orthogonal to that of cGAMP.
Compound 53 triggers outward shifts of transmembrane helices in the dimer, and induces inter-dimer interactions between these helices to mediate the formation of the high-order oligomer.

Physicochemical Properties

M.Wt 490.883
Formula C25H19ClF4N2O2
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-(2-Chloro-6-fluorobenzyl)-3,3-dimethyl-2-oxo-N-(2,4,6-trifluorobenzyl)indoline-6-carboxamide

References

1. Lu D, et al. Nature. 2022 Apr 6. doi: 10.1038/s41586-022-04559-7.

2. David C Pryde, et al. Eur J Med Chem. 2021 Jan 1;209:112869.

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