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首页-小分子抑制剂&激动剂-Others-Other Targets-TQ416
TQ416

Chemical Structure : TQ416

CAS No.: 950388-70-2

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TQ416 (TQ-416)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    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.

    物理化学性质&存储条件

    分子量 363.48
    分子式 C21H21N3OS
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    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

    参考文献

    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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