MG-132, a peptide aldehyde, is a novel, specific, potent, reversible, and cell-permeable inhibitor of proteasome with IC50 of 100 nM in a cell-free assay, and also inhibits calpain with IC50 of 1.2 μM.
Oprozomib (formerly known as ONX 0912 and PR 047) is a novel, potent, and orally bioavailable small molecule inhibitor for chymotrypsin-like (CT)-L activity of 20S proteasome β5/LMP7 with potential antitumor activity.
ONX-0914 (also known as ONX0914; PR957) is a selective inhibitor of LMP7 and LMP2 subunits of immunoproteasomes with the potential to be used in autoimmune diseases including rheumatoid arthritis, inflammatory bowel disease and lupus.
Ixazomib citrate (MLN9708; MLN-9708; MLN 9708), the citrate salt and orally bioavailable prodrug of Ixazomib (MMLN2238; MMLN-2238), is a selective inhibitor of 20S proteasome (IC50 = 3.4 nM) with potential anticancer activity.
Epoxomicin (formerly also known as BU-4061T) is a novel, potent, selective, cell-permeable and irreversible proteasome inhibitor with anti-inflammatory activity, it inhibits primarily the CH-L activity of the 20S proteasome, while T-L and PGPH catalytic activities are also inhibited at 100- and 1000-fold reduced rate.
VR23 (VR-23; VR 23) is a highly potent and selective inhibitor of trypsin-like proteasome with potential antitumor activity.
Ixazomib (formerly also known as MLN-2238) is a novel, potent, selective and reversible proteasome inhibitor (PI) with potential antineoplastic activity.
Carfilzomib (formerly also known as PR-171; trade name: Kyprolis) is a novel, potent, and irreversible proteasome inhibitor with potential antineoplastic activity.
MLN9708 (also known as ixazomib citrate; MLN-9708; trade name Ninlaro), the citrate salt of Ixazomib (MMLN2238; MMLN-2238), is a prodrug of Ixazomib (MMLN-2238) which is an orally bioavailable and 2nd generation proteasome inhibitor (PI) with potential antineoplastic activity.
Delanzomib (formerly known as CEP-18770) is a novel, potent, and orally bioactive inhibitor of the chymotrypsin-like (CL) activity of proteasome with potential antineoplastic activity.