- 20S proteasome
20S-proteasome Selective Inhibitors
|Catalog No.||Product Name||Information||Selective / Pan||IC50 / Ki|
Bortezomib (PS-341) is a potent 20S proteasome inhibitor with Ki of 0.6 nM.
|Selective||20S proteasome, Ki: 0.6 nM|
MLN9708 immediately hydrolyzed to MLN2238, the biologically active form, on exposure to aqueous solutions or plasma. MLN2238 inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50/Ki of 3.4 nM/0.93 nM, less potent to β1 and little activity to β2. Phase 3.
|Selective||20S proteasome, IC50: 3.4 nM; 20S proteasome, Ki: 0.93 nM|
MLN2238 inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50 and Ki of 3.4 nM and 0.93 nM, respectively, also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites, with IC50 of 31 and 3500 nM. Phase 3.
|Selective||20S proteasome, Ki: 0.93 nM; 20S proteasome, IC50: 3.4 nM|
CEP-18770 (Delanzomib) is an orally active inhibitor of the chymotrypsin-like activity of proteasome with IC50 of 3.8 nM, with only marginal inhibition of the tryptic and peptidylglutamyl activities of the proteosome. Phase 1/2.
|Selective||Chymotrypsin-like proteasome, IC50: 3.8 nM|
PI-1840 is a reversible and selective chymotrypsin-like (CT-L) inhibitor with IC50 of 27 nM with little effects on the other two major proteasome proteolytic activities, trypsin-like (T-L) and postglutamyl-peptide-hydrolysis-like (PGPH-L).
|Selective||Chymotrypsin-like proteasome, IC50: 27 nM|
|S7049||Oprozomib (ONX 0912)||
Oprozomib (ONX 0912) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM. Phase 1/2.
|Selective||20S proteasome β5, IC50: 36 nM; 20S proteasome LMP7, IC50: 82 nM|
Celastrol is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM.
|Selective||20S proteasome, IC50: 2.5 μM; 20S proteasome, :|
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