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TG2-179-1

Chemical Structure : TG2-179-1

CAS No.: 1135023-19-6

TG2-179-1 (BAP1 inhibitor)

Catalog No.: PC-20004Not For Human Use, Lab Use Only.

TG2-179-1 is a potent, selective and covalently inhibitor of deubiquitinase (DUB) BRCA1-associated protein-1 (BAP1), covalently binds to the active site of BAP1 (Cys91), exhibits potent cytotoxic activity against colon cancer cells.

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    Biological Activity

    TG2-179-1 is a potent, selective and covalently inhibitor of deubiquitinase (DUB) BRCA1-associated protein-1 (BAP1), covalently binds to the active site of BAP1 (Cys91), exhibits potent cytotoxic activity against colon cancer cells.
    TG2-179-1 has potent cytotoxic activity against colon cancer cells with IC50 of <10 uM against HCT116, HT29 and SW48 cells, and BAP1-proficient cells are more sensitive to TG2-179-1 than BAP1-deficient cells.
    TG2-179-1 exerts its cytotoxic activity against colon cancer cells as well as other types of cancer cells, such as mesothelioma and ccRCC, by targeting BAP1.
    TG2-179-1 induces replication defects in colon cancer cells and increases the level of γ-H2AX in a dose-dependent manner in HCT116 cells, which is similar to BAP1 depletion.
    TG2-179-1 inhibits the growth of colon tumors in mice.

    Physicochemical Properties

    M.Wt 484.95
    Formula C22H14ClFN4O2S2
    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

    2-[[5-(4-chlorophenyl)-1,3,4-oxadiazol-2-yl]sulfanyl]-N-[3-cyano-4-(4-fluorophenyl)-5-methylthiophen-2-yl]acetamide

    References

    1. Kang M, et al. Sci Rep. 2023 Feb 8;13(1):2264.

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