|Description||Epoxomicin is a potent anti-tumor agent isolated from Actinomycetes that is used as a selective and irreversible inhibitor of the 20S proteasome. It inhibits proteasome activity in cell growth assays with an IC50 value of 4 nM and demonstrates potent cytotoxicity against B16-F10, HCT116, and Moser solid tumor cells, as well as P388 and K562 leukemia cells with IC50 values ranging from 2-44 nM. By inhibiting osteoblast proteasome activity, epoxomicin stimulates bone formation at concentrations as low as 10 nM. Intraperitoneal injection of 1.5 mg/kg epoxomicin given daily for two weeks induces Parkinson’s-like symptoms in rats and addition of 100 nM epoxomicin to rat ventral midbrain cultures results in apoptosis specific to dopaminergic neurons. Epoxomicin-induced parkinsonism can be a useful model to examine mechanisms and therapies for the disease.|
Carfilzomib is a tetrapeptide epoxyketone and an analog of epoxomicin, acting as a selective proteasome inhibitor, such as the chymotrypsin-like β5 subunit of t...
Cysteine Protease inhibitor
Cysteine Protease inhibitor is a inhibitor of cysteine protease.
Oprozomibm, also known as ONX 0912 and PR 047, is an orally bioavailable proteasome inhibitor with potential antineoplastic activity. ONX 0912 inhibits the act...
Delanzomib, also known as CEP-18770, is An orally bioavailable synthetic P2 threonine boronic acid inhibitor of the chymotrypsin-like activity of the proteasom...
MG-132(S,R,S) is a reversible, cell permeable and selective tripeptide aldehyde proteasome inhibitor (IC50 = 0.22 μM), the most potent stereoisomer of MG-132. I...
Bortezomib (PS-341) is a potent 20S proteasome inhibitor with Ki of 0.6 nM.
PMSF is an irreversible serine/cysteine protease inhibitor.
ONX 0914 is an immunoproteasome inhibitor with potential treatment applications in autoimmune disorders, such as rheumatoid arthritis, inflammatory bowel diseas...