Proteasome

Bortezomib is a highly selective, reversible inhibitor of the 26S proteasome

MLN2238 is a potent reversible and specific β5 site of the 20S proteasome inhibitor with an IC50 value of 3.4 nM.

Ixazomib Citrate (MLN9708) Analogue is a proteasome inhibitor, which inhibits the activity of the proteasome, blocking the targeted proteolysis normally performed by the proteasome.

MG-132 is a potent cell-permeable inhibitor of proteasome (IC50 = 100 nM) and calpain (IC50 = 1.2 μM).

CEP-18770 is a novel orally active proteasome inhibitor with a favorable tumor selectivity profile for the treatment of MM and other malignancies responsive to proteasome inhibition.

PR-171 (Carfilzomib) is a tetrapeptide epoxyketone and a selective proteasome inhibitor. It is an analog of epoxomicin.

MG-115 is a potent, reversible peptide aldehyde inhibitor of proteasome chymotrypsin-like and caspase-like activities. It induces p53 dependent apoptosis.

ONX 0914 is an immunoproteasome inhibitor with potential treatment applications in autoimmune disorders, such as rheumatoid arthritis, inflammatory bowel disease and lupus. ONX 0914 was designed to be a potent inhibitor of the immunoproteasome with minimal cross-reactivity for the constitutive proteasome.

VR23 is a small molecule that potently inhibited the activities of trypsin-like proteasomes (IC50 = 1 nM), chymotrypsin-like proteasomes (IC50 = 50-100 nM), and caspase-like proteasomes (IC50 = 3uM).

PSI is a proteasome inhibitor that inhibits chymotrypsin-like activity of the proteasome.

PI-1840 is a novel noncovalent and rapidly reversible proteasome inhibitor with anti-tumor activity.

AM 114, a derivative of boronic chalcone, is a potent small-molecule inhibitor of the proteasome that inhibits the chymotrypsin-like activity of the 20S proteasome, with a value of 50% inhibition concentration IC50 of approximately 1 uM, resulting in a significant accumulation of ubiquitinated p53 and other cellular proteins in whole cells without significantly disrupting the interaction of p53 and murine double minute 2 (mdm2) proteins.

Ixazomib citrate (MLN9708) is a reversible inhibitor of the chymotrypsin-like proteolytic β5 site of the 20S proteasome with an IC50 of 3.4 nM and a Ki of 0.93 nM.

Isovalerylcarnitine is a product of the catabolism of L-leucine. It increases calpain activity.