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Zetomipzomib

Chemical Structure : Zetomipzomib

CAS No.: 1629677-75-3

Zetomipzomib (KZR-616, KZR616)

Catalog No.: PC-38434Not For Human Use, Lab Use Only.

Zetomipzomib (KZR-616) is a first-in-class inhibitor of immunoproteasome, dually inhibits immunoproteasome subunits LMP7 (IC50, 39/57 nM, hLMP7/mLMP7) and LMP2 (IC50, 131/179 nM, hLMP2/mLMP2).

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    Biological Activity

    Zetomipzomib (KZR-616) is a first-in-class inhibitor of immunoproteasome, dually inhibits immunoproteasome subunits LMP7 (IC50, 39/57 nM, hLMP7/mLMP7) and LMP2 (IC50, 131/179 nM, hLMP2/mLMP2).
    Zetomipzomib (KZR-616) also potently inhibits MECL-1 subunit (IC50=623 nM) and constitutive proteasome β5 subunit (IC50=688 nM), and maintains LMP7 and LMP2 selective inhibition in MOLT-4 cells.
    Zetomipzomib (KZR-616) exhibits potent cytokine expression inhibition and in vivo efficacy in an inflammatory disease model.

    Physicochemical Properties

    M.Wt 586.68
    Formula C30H42N4O8
    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

    (2S,3R)-N-((S)-3-(cyclopent-1-en-1-yl)-1-((R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-((S)-2-(2-morpholinoacetamido)propanamido)propanamide

    References

    1. Johnson HWB, et al. J Med Chem. 2018 Dec 27;61(24):11127-11143.

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