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ZH97

Chemical Structure : ZH97

CAS No.: 3033551-45-7

ZH97 (BFL-1 selective inhibitor)

Catalog No.: PC-73235Not For Human Use, Lab Use Only.

ZH97 is a selective and covalent small-molecule inhibitor of BFL-1 protein with binding Ki of 0.41 uM, >200-fold selectivity over MCL-1.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    ZH97 is a selective and covalent small-molecule inhibitor of BFL-1 protein with binding Ki of 0.41 uM, >200-fold selectivity over MCL-1.
    ZH97 does not bind to BCL-xL, BCL-2, TEAD2, TEAD4, MDM2, MDMX, BRD2 BD1, BRD2 BD2, BRD3 BD1, BRD3 BD2, BCL9, PD1/PD-L1 (Ki>400 uM).
    ZH97 modifies BFL-1 at the C55 residue, blocks BFL-1/BID interaction in vitro.
    ZH97 dose-dependently increased cytoplasmic cytochrome c level in U937 cells, has cell growth inhibition with IC50 of 2.8 uM, 5.5 uM, 7.7 uM, 6.8 uM, and 3.9 uM in U937, Kasumi-1, K562, MM.1S, and MV4-11 cell lines, respectively.
    ZH97 inhibits BFL-1/PUMA interaction in cell lysate and is effective in cancer cells that harboring high
    expression level of BFL-1.

    Physicochemical Properties

    M.Wt 440.522
    Formula C27H25FN4O
    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

    1-(4-(2-benzyl-6-(3-fluorophenyl)-2H-indazol-3-yl)piperazin-1-yl)prop-2-en-1-one

    References

    1. Xuexin Feng, et al. European Journal of Medicinal Chemistry 236 (2022) 114327

    2. Karson J Kump, et al. J Med Chem. 2020 Mar 12;63(5):2489-2510.

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