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HOIPIN-8

Chemical Structure : HOIPIN-8

CAS No.: 2519537-69-8

HOIPIN-8 (HOIP inhibitor-8)

Catalog No.: PC-35959Not For Human Use, Lab Use Only.

HOIPIN-8 (HOIP inhibitor-8) is a potent chemical inhibitor of linear ubiquitin chain assembly complex (LUBAC, IC50=11 nM), specifically generates Met1-linked linear ubiquitin chains through the ubiquitin ligase activity in HOIP, and activates the NF-kB pathway.

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    Biological Activity

    HOIPIN-8 (HOIP inhibitor-8) is a potent chemical inhibitor of linear ubiquitin chain assembly complex (LUBAC, IC50=11 nM), specifically generates Met1-linked linear ubiquitin chains through the ubiquitin ligase activity in HOIP, and activates the NF-kB pathway.
    HOIPIN-8 suppresses the linear ubiquitination activity by recombinant LUBAC, displays 255-fold increased potency over that of HOIPIN-1 (JTP-0819958, IC50=2.8 uM).
    HOIPIN-8 also shows 10-fold and 4-fold enhanced inhibitory activities on LUBAC- and TNF-a-induced NF-kB activation respectively, without cytotoxicity.
    HOIPIN-8 is a powerful tool to explore the physiological functions of LUBAC.

    Physicochemical Properties

    M.Wt 456.385
    Formula C23H15F2N4NaO3
    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

    Sodium (E)-2-(3-(2,6-difluoro-4-(1H-pyrazol-4-yl)phenyl)-3-oxoprop-1-en-1-yl)-4-(1-methyl-1H-pyrazol-4-yl)benzoate

    References

    1. Katsuya K, et al. Biochem Biophys Res Commun. 2019 Jan 2. pii: S0006-291X(18)32846-8.

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