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YC137

Chemical Structure : YC137

CAS No.: 810659-53-1

YC137 (YC-137)

Catalog No.: PC-25524Not For Human Use, Lab Use Only.

YC137 is a specific small molecule inhibitor of Bcl-2 with Ki of 1.3 uM, with no affinity for Bcl-xL (Ki>100 uM), inhibits the binding of the Bid BH3 peptide to Bcl-2, thus disrupting an interaction essential for the antiapoptotic activity of Bcl-2.

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    Biological Activity

    YC137 is a specific small molecule inhibitor of Bcl-2 with Ki of 1.3 uM, with no affinity for Bcl-xL (Ki>100 uM), inhibits the binding of the Bid BH3 peptide to Bcl-2, thus disrupting an interaction essential for the antiapoptotic activity of Bcl-2.
    YC137 induced apoptosis of Bcl-2-transfected cells in a dose-dependent manner.
    YC137 induces apoptosis in breast cancer cells that express high levels of Bcl-2 but does not have any effect on normal hematopoietic progenitors, peripheral blood mononuclear cells (PBMCs), small intestine epithelial cells, and myoblasts.
    Combination of guanine arabinoside and Bcl-2 inhibitor YC137 overcomes the cytarabine resistance in HL-60 leukemia cell line.

    Physicochemical Properties

    M.Wt 511.57
    Formula C24H21N3O6S2
    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-((4,9-dioxo-4,9-dihydronaphtho[2,3-d]thiazol-2-yl)amino)phenyl (methoxycarbonyl)-L-methioninate

    References

    1. Nishi R, et al. Cancer Sci. 2013 Apr;104(4):502-7.

    2. Real PJ, et al. Cancer Res. 2004 Nov 1;64(21):7947-53.

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