Description: Marizomib (ML858) is a novel irreversible brain-permeable proteasome inhibitor that inhibits CT-L (beta5), CT-T-laspase-like (C-L, beta1), and trypsin-like (T-L, beta2) 20S proteasomes with IC50s of 3.5, 28, and 430 nM, respectively. Target: Proteasome. Smiles:...

Potent, irreversible inhibitor of all the 3 proteolytic activities of the mammalian 20S proteasome. beta5 subunit: chymotrypsin-like (EC50 = 3.5nM) beta2 subunit: trypsin-like (EC50 = 28nM) beta1 subunit: caspase-like or peptidyl-glutamyl peptide-hydrolyzing (PGPH) (EC50 = 430nM) Potent anticancer compound. Triggers...

Salinosporamide A is a natural proteasome inhibitor. It is a beta-lactone-gamma-lactam that irreversibly inhibits all three protease activities within the proteasome (IC50s = 3.5, 28, and 430 nM for beta5 (chymotrypsin), beta2 (macropain), and beta1 (C5) subunits, respectively), both in vitro and in vivo....