Chemical Structure : TDI-8304
货号: 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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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.
分子量 | 597.75 | |
分子式 | C32H47N5O6 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Zhan W, et al. Angew. Chem. Int. Ed. Engl. 2021;60:9279–9283.
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