GSK3494245 is a selective inhibitor of the chymotrypsin-like activity of the Leishmania donovani proteasome, targeting a site between the β4 and β5 subunits with an IC50 of 0.16 μM. This compound demonstrates moderate inhibitory effects on the chymotrypsin-like activity of human proteasomes, exhibiting IC50 values of 13 µM in purified 26S and 40 µM in enriched THP-1 extracts. GSK3494245's potent activity and favorable biosafety profile make it a valuable tool for research in parasitology and potential therapeutic applications against leishmaniasis.
GSK3494245 is a selective inhibitor of the chymotrypsin-like activity of the Leishmania donovani proteasome, targeting a site between the β4 and β5 subunits with an IC50 of 0.16 μM. This compound demonstrates moderate inhibitory effects on the chymotrypsin-like activity of human proteasomes, exhibiting IC50 values of 13 µM in purified 26S and 40 µM in enriched THP-1 extracts. GSK3494245's potent activity and favorable biosafety profile make it a valuable tool for research in parasitology and potential therapeutic applications against leishmaniasis.
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