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mCMY020

Chemical Structure : mCMY020

CAS No.:

mCMY020 (mCMY 020)

Catalog No.: PC-21290Not For Human Use, Lab Use Only.

mCMY020 is a potent, specific and covalent inhibitor of TEAD transcriptional activity with IC50 of 91.9-468.6 nM for TEAD1-4.

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    Biological Activity

    mCMY020 is a potent, specific and covalent inhibitor of TEAD transcriptional activity with IC50 of 91.9-468.6 nM for TEAD1-4.
    mCMY020 occupies the palmitoylation sites and form covalent adducts with recombinant preparations of TEAD1, TEAD2, TEAD3 and TEAD4.
    mCMY020 does not significantly inhibit the catalytic activity of EGFR, BTK, and SARS-CoV-2 main protease (MPro).
    mCMY020 inhibits TEAD-dependent transcriptional program (IC50=162.1 nM, MCF-7 cell line) and cell proliferation, markedly decreases the levels of the YAP-controlled transcripts CYR61, CTGF, and ANKRD1.
    mCMY020 inhibits proliferation in Hippo pathway deficient cancers, potently inhibits NCI-H226 (NF2-deficient) and NCI-H2052 (homozygous for NF2 inactivating mutations) malignant mesotheliomas with IC50 of 261.3 nM and 228.7 nM, respectively.

    Physicochemical Properties

    M.Wt 364.42
    Formula C21H21FN4O
    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

    N-(5-(4-cyclohexylphenyl)pyrazolo[1,5-a]pyrimidin-3-yl)-2-fluoroacrylamide

    References

    1. Kayla Nutsch, et al. RSC Chem Biol. 2023 Aug 29;4(11):894-905.

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