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MRK-003

Chemical Structure : MRK-003

CAS No.: 623165-93-5

MRK-003 (MRK 003;MRK003)

Catalog No.: PC-70070Not For Human Use, Lab Use Only.

MRK-003 (MRK003) is a potent γ-secretase inhibitor with IC50 of 0.4 nM, inhibition of Aβ secretion from SH-SY5Y SPA4CT cells.

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    Biological Activity

    MRK-003 (MRK003) is a potent γ-secretase inhibitor with IC50 of 0.4 nM, inhibition of Aβ secretion from SH-SY5Y SPA4CT cells.
    MRK-003 inhibits the γ-secretase-mediated cleavage of the Notch receptor, reduces tumor cell proliferation, inhibits serum independence, and induces apoptosis in vitro and in vivo using mouse xenograft models.

    Physicochemical Properties

    M.Wt 551.59
    Formula C25H31F6N3O2S
    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

    (3R,6'S,9'R)-5-(2,2,2-trifluoroethyl)-2'-((E)-3-(4-(trifluoromethyl)piperidin-1-yl)prop-1-en-1-yl)-5',6',7',8',9',10'-hexahydrospiro[[1,2,5]thiadiazolidine-3,11'-[6,9]methanobenzo[8]annulene] 1,1-dioxide

    References

    1. Lewis HD, et al. Chem Biol. 2007 Feb;14(2):209-19.

    2. Sparey T, et al. Bioorg Med Chem Lett. 2005 Oct 1;15(19):4212-6.

    3. Konishi J, et al. Cancer Res. 2007 Sep 1;67(17):8051-7.

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