ct-l

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.

PI-1840(IC50 = 27 nM)is a reversible and selective chymotrypsin-like (CT-L) inhibitor, with little proteasome proteolytic effects on trypsin-like (T-L) and postglutamyl-peptide-hydrolysis-like (PGPH-L).

Marizomib is a novel irreversible brain-permeable proteasome inhibitor that inhibits CT-L (β5), CT-T-laspase-like (C-L, β1), and trypsin-like (T-L, β2) 20S proteasomes with IC50s of 3.5, 28, and 430 nM.[3]

BC-23 (NSC 45382) is a potent proteasome inhibitor with antitumor and antimicrobial activity, inhibiting the CT-L activity of the proteasome and used in the study of leukemias, lymphomas, gliomas, breast cancer, and small cell lung cancer.

Enzyme-IN-1 (compound 1), a peptide-based inhibitor of N-terminal nucleophile (Ntn) hydrolases, specifically targets and inhibits the chymotrypsin-like activity (CT-L) of the 20S proteasome. This compound may possess potential anti-inflammatory properties [1].