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TMPRSS6 inhibitor 8

Chemical Structure : TMPRSS6 inhibitor 8

CAS No.: 2088415-78-3

TMPRSS6 inhibitor 8 (TMPRSS6-IN-8)

Catalog No.: PC-73085Not For Human Use, Lab Use Only.

TMPRSS6 inhibitor 8 (TMPRSS6-IN-8) is a highly potent (IC50=8.1 nM), peptidomimetic inhibitor of TMPRSS6 (matriptase-2).

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    Biological Activity

    TMPRSS6 inhibitor 8 (TMPRSS6-IN-8) is a highly potent (IC50=8.1 nM), peptidomimetic inhibitor of TMPRSS6 (matriptase-2).
    TMPRSS6-IN-8 inhibits two closely related TTSPs (matriptase and hepsin, IC50 52 nM and 16 nM, respectively), weakly inhibits thrombin and factor Xa and has no inhibitory activity toward furin.
    TMPRSS6-IN-8 forms a reversible covalent bond with TMPRSS6.
    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.
     

    Physicochemical Properties

    M.Wt 676.855
    Formula C33H40N8O4S2
    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)-N-((S)-1-(benzo[d]thiazol-2-yl)-5-guanidino-1-oxopentan-2-yl)-3-methyl-2-((S)-2-(3-phenylpropanamido)-3-(thiazol-4-yl)propanamido)butanamide

    References

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

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