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TQ416

Chemical Structure : TQ416

CAS No.: 950388-70-2

TQ416 (TQ-416)

Catalog No.: PC-26444Not For Human Use, Lab Use Only.

TQ416 is a small molecule paraoxonase 2 (PON2) inhibitor, restores NF-κB transcriptional activity suppressed by N-(3-oxododecanoyl)-L-homoserine lactone (3OC12HSL, C12) with IC50 of 400 nM, rescues 3OC12HSL-induced cell death.

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    Biological Activity

    TQ416 is a small molecule paraoxonase 2 (PON2) inhibitor, restores NF-κB transcriptional activity suppressed by N-(3-oxododecanoyl)-L-homoserine lactone (3OC12HSL, C12) with IC50 of 400 nM, rescues 3OC12HSL-induced cell death.
    TQ416 inhibits 3OC12HSL hydrolysis and to prevent cytosolic acidification in HEK293T cells.
    TQ416 (0.5-5 uM) rescues 3OC12HSL-induced cell death through PON2 inhibition.
    Treatment with C12-HSL at 100 μM for 4 h markedly decreased MUC2 production in LS174T cells and TQ416 (1 μM) completely restored this decrease.
    TQ416 significantly attenuated the production of IL-8 and IL-1β compared with the C12-HSL alone in LS174T cells.
    TQ416 fully restored NF-κB transcriptional responses in LPS-stimulated FRT-NF-κB cells with IC50 of 400 nM.
    TQ416 inhibits N-(3-oxo-dodecanoyl) homoserine lactone (C12) action to restore cytokine secretion in LPS-stimulated cells.

    Physicochemical Properties

    M.Wt 363.48
    Formula C21H21N3OS
    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

    5,9-dimethyl-1-((2-(p-tolyloxy)ethyl)thio)-[1,2,4]triazolo[4,3-a]quinoline

    References

    1. Tao S, et al. Sci Rep. 2016 Jul 1;6:28778.

    2. Tao S, et al. Life Sci. 2018 May 15;201:81-88.

    3. Cathleen D Valentine, et al. Cell Microbiol. 2014 Jan;16(1):1-14.

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