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TMPRSS6 inhibitor Cpd-B

Chemical Structure : TMPRSS6 inhibitor Cpd-B

CAS No.: 2702322-34-5

TMPRSS6 inhibitor Cpd-B

Catalog No.: PC-73086Not For Human Use, Lab Use Only.

TMPRSS6 inhibitor Cpd-B (TMPRSS6-IN-Cpd-B) is a highly potent (IC50=7.6 nM), specific small molecule inhibitor of TMPRSS6 (matriptase-2).

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    Biological Activity

    TMPRSS6 inhibitor Cpd-B (TMPRSS6-IN-Cpd-B) is a highly potent (IC50=7.6 nM), specific small molecule inhibitor of TMPRSS6 (matriptase-2).
    TMPRSS6 inhibitor Cpd-B shows no activity toward furin, wekaly inhibits other TTSP family members matriptase and hepsin, as well as factor Xa and thrombin.
    TMPRSS6 inhibitor Cpd-B demonstrates cellualr IC50 (144 nM) in cell media of TMPRSS6-transfected HEK293 cells with no cytotoxicity, and no negatively affect TMPRSS6 plasma membrane localization.
    Inhibiting TMPRSS6 proteolytic activity prevents cleavage of hemojuvelin (HJV) in HeLa cells (IC50=267 nM).
    TMPRSS6 inhibition increases hepcidin encoding gene (HAMP) expression in HepG2 cells and human primary hepatocytes.
    TMPRSS6, also known as matriptase-2, is a TTSP almost exclusively expressed at the surface of hepatocytes in the liver, and plays a key role in iron homeostasis via modulation of hepcidin expression.

    Physicochemical Properties

    M.Wt 636.265
    Formula C28H25BBrF2N7O3
    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

    (4-(6-((3-(aminomethyl)benzyl)amino)-9-(3-((4-bromophenyl)amino)-3-oxopropyl)-9H-purin-8-yl)-3,5-difluorophenyl)boronic acid

    References

    1. Béliveau F, et al. Cell Chem Biol. 2019 Nov 21;26(11):1559-1572.e9.

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