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hTG2 inhibitor VA4

Chemical Structure : hTG2 inhibitor VA4

CAS No.: 2088001-23-2

hTG2 inhibitor VA4 (VA4)

Catalog No.: PC-61052Not For Human Use, Lab Use Only.

hTG2 inhibitor VA4(VA4) is a novel potent, irreversible inhibitor of human tissue transglutaminase (hTG2) with Ki of 12.9 uM, allosterically abolishs its GTP binding ability with a high degree of selectivity and efficiency.

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    Biological Activity

    hTG2 inhibitor VA4 (VA4) is a novel potent, irreversible inhibitor of human tissue transglutaminase (hTG2) with Ki of 12.9 uM, allosterically abolishs its GTP binding ability with a high degree of selectivity and efficiency.
    hTG2 inhibitor VA4 inhibits both the transamidation and GTP binding activity of hTG2 in a cellular context.
    hTG2 inhibitor VA4 inhibits epidermal cancer stem cell invasion with EC50 of 3.9 uM.

    Physicochemical Properties

    M.Wt 635.78
    Formula C33H41N5O6S
    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

    (S)-Benzyl (6-Acrylamido-1-(4-((5-(dimethylamino)naphthalen-1-yl)sulfonyl)piperazin-1-yl)-1-oxohexan-2-yl)carbamate

    References

    1. Akbar A, et al. J Med Chem. 2017 Sep 28;60(18):7910-7927.

    2. Feola J, et al. Brain Res. 2017 Aug 1;1668:1-11.

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