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PPI-2458

Chemical Structure : PPI-2458

CAS No.: 431077-35-9

PPI-2458 (PPI2458)

Catalog No.: PC-63319Not For Human Use, Lab Use Only.

PPI-2458 is potent, specific, irreversible methionine aminopeptidase-2 (MetAP-2) inhibitor with IC50 of 0.2 nM, inhibits growth inhibition of HFLS-RA and HUVEC with IC50 of 0.04 nM.

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

    Biological Activity

    PPI-2458 is potent, specific, irreversible methionine aminopeptidase-2 (MetAP-2) inhibitor with IC50 of 0.2 nM, inhibits growth inhibition of HFLS-RA and HUVEC with IC50 of 0.04 nM.
    PPI-2458 significantly attenuates paw swelling when therapeutically administered after the onset of chronic disease in rat model of peptidoglycan-polysaccharide-induced arthritis.
    PPI-2458 exhibits potent antiproliferative activity on NHL lines in vitro (GI50=0.2-1.9 nM) and oral antitumor activity in vivo.

    Physicochemical Properties

    M.Wt 424.53
    Formula C22H36N2O6
    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

    (3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate

    References

    1. Bernier SG, et al. Proc Natl Acad Sci U S A. 2004 Jul 20;101(29):10768-73.

    2. Hannig G, et al. Int J Oncol. 2006 Apr;28(4):955-63.

    3. Cooper AC, et al. Clin Cancer Res. 2006 Apr 15;12(8):2583-90.

    4. Hannig G, et al. Arthritis Rheum. 2007 Mar;56(3):850-60.

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