epoxyketone

Oprozomib (PR-047) (ONX 0912) , an inhibitor for CT-L activity of 20S proteasome β5(IC50=36 nM) LMP7(IC50=82 nM), is orally bioavailable. Oprozomib also has potential antineoplastic activity.

PR-924 is a selective inhibitor of tripeptide epoxyketone immunoproteasome subunit LMP-7 (IC50: 22 nM). PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities. PR-924 covalently modifies proteasomal N-terminal threonine active sites.

Proteasome-IN-7 (Compound 6f) is a macrolactam-based epoxyketone proteasome inhibitor with an IC50 value of 37.92 nM against the 20S proteasome ChT-L subunit. It exhibits potent antiproliferative effects on multiple myeloma, acute lymphoblastic leukemia, and non-small cell lung cancer.

Epoxomicin (BU-4061T,Aids010837) is a selective proteasome inhibitor with anti-inflammatory activity, 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.