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P217564

Chemical Structure : P217564

CAS No.: 2773337-26-9

P217564 (P0217564;P 217564)

Catalog No.: PC-62574Not For Human Use, Lab Use Only.

P 217564 is a potent, selective, irreversible second generation inhibitor of USP7 with IC50 of 0.48 uM, with similar potency against USP47 and no significant activity aginst other DUBs.

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

    Biological Activity

    P217564 is a potent, selective, irreversible second generation inhibitor of USP7 with IC50 of 0.48 uM, with similar potency against USP47 and no significant activity aginst other DUBs.
    P217564 exhibits 10-fold increase in potency compared to P5091, selectively targets the catalytic cleft of USP7 and modifies its active site cysteine (C223) by forming a covalent adduct.
    P217564 downregulates Foxp3 and Tip60 in Treg cells and impairs Treg functions, increases polyubiquitination of Foxp3, Tip60 and USP7, induces dose- and time-dependent apoptosis of Jurkat cells.

    Physicochemical Properties

    M.Wt 447.3
    Formula C16H12Cl2N2O5S2
    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

    Methyl (E)-4-(5-((2,3-dichlorophenyl)thio)-4-nitrothiophene-2-carboxamido)but-2-enoate

    References

    1. Wang F, et al. PLoS One. 2017 Dec 13;12(12):e0189744.

    2. Wang L, et al. EBioMedicine. 2016 Nov;13:99-112.

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