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TDI-8304

Chemical Structure : TDI-8304

CAS No.: 2307262-96-8

TDI-8304 (TDI 8304)

Catalog No.: PC-21553Not For Human Use, Lab Use Only.

TDI-8304 is a highly selective, macrocyclic peptide inhibitor of malaria parasite Plasmodium falciparum proteasome (Pf20S) with IC50 of 0.06 uM, shows high potency against P. falciparum strain Pf 3D7 (EC50=0.009 uM).

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    Biological Activity

    TDI-8304 is a highly selective, macrocyclic peptide inhibitor of malaria parasite Plasmodium falciparum proteasome (Pf20S) with IC50 of 0.06 uM, shows high potency against P. falciparum strain Pf 3D7 (EC50=0.009 uM).
    TDI-8304 displays high selectivity over human constitutive proteasome (c-20S) and human immunoproteasome (i-20S) with IC50 of >80 uM.
    TDI-8304 demonstrates specific, time-dependent inhibition of the β5 subunit of the Plasmodium falciparum proteasome, kills artemisinin-sensitive and artemisinin-resistant P. falciparum isolates in vitro.
    TDI-8304 reduces parasitemia in humanized, P. falciparum-infected mice.

    Physicochemical Properties

    M.Wt 597.75
    Formula C32H47N5O6
    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

    2-Oxa-8,11-diazabicyclo[13.3.1]nonadeca-1(19),15,17-triene-7-carboxamide, N-cyclopentyl-10-[2-(4-morpholinyl)ethyl]-9,12-dioxo-13-(2-oxo-1-pyrrolidinyl)-, (7S,10S,13S)-

    References

    1. Zhan W, et al. Angew. Chem. Int. Ed. Engl. 2021;60:9279–9283.

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