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TED-642

Chemical Structure : TED-642

CAS No.: 3034773-95-7

TED-642 (TED642)

Catalog No.: PC-49697Not For Human Use, Lab Use Only.

TED-642 (TED642) is a potent, covalent, pan-TEAD-YAP1 antagonist, inhibits TEAD1/2/4 binding to YAP with IC50 of 0.9-1.2 uM.

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    Biological Activity

    TED-642 (TED642) is a potent, covalent, pan-TEAD-YAP1 antagonist, inhibits TEAD1/2/4 binding to YAP with IC50 of 0.9-1.2 uM.
    TED-642 forms a covalent bond with the central pocket cysteine of TEADs (TEAD4, Cys-367).
    TED-642 inhibited the binding of FAM-YAP1 60-99 to TEAD4 with an IC50 of 1.1 uM, with similar IC50 values for TEAD1 and TEAD2 to FAM-YAP 60-99.
    TED-642 inhibits TEAD transcriptional activity (CTGF transcript level) in breast cancer cell MDA-MB-468 with IC50 of 0.6 uM, inhibits TEAD1-4 transcriptional activity in HEK-293 cells with IC50 of 2.2-5.1 uM.
    TED-642 inhibits cell proliferation of osteosarcoma cell lines SaOS-2 and SaOS-LM7 with IC50 of 0.1 and 0.2 uM, respectively.

    Physicochemical Properties

    M.Wt 303.29
    Formula C16H12F3N3
    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-((3-(trifluoromethyl)phenyl)amino)isoindoline-2-carbonitrile

    References

    1. Bum-Erdene K, et al. J Med Chem. 2023 Jan 12;66(1):266-284.

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