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STING inhibitor 18

Chemical Structure : STING inhibitor 18

CAS No.: 2377104-08-8

STING inhibitor 18

Catalog No.: PC-36011Not For Human Use, Lab Use Only.

STING inhibitor 18 is a novel cGAMP competitive ligand (antagonist) of the inactive form of STING with IC50 of 68 nM in the HAQ STING cGAMP displacement assays.

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    Biological Activity

    STING inhibitor 18 is a novel cGAMP competitive ligand (antagonist) of the inactive form of STING with IC50 of 68 nM in the HAQ STING cGAMP displacement assays.
    STING inhibitor 18 does not stimulate IFNβ production (EC50=>30000 nM), but modestly inhibits cGAMP-induced IFNβ production (EC50=1.1 uM).
    STING inhibitor 18 demonstrates slow dissociation kinetics, good oral bioavailability, and ability to inhibit cGAMP dependent signaling in vitro.

    Physicochemical Properties

    M.Wt 509.958
    Formula C28H25ClFNO5
    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

    (3S,4S)-2-(4-(tert-butyl)-3-chlorophenyl)-3-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-7-fluoro-1-oxo-1,2,3,4-tetrahydroisoquinoline-4-carboxylic acid

    References

    1. Siu T, et al. ACS Med Chem Lett. 2018 Dec 6;10(1):92-97.

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