|Description||MLN-2238 is the biologically active form of MLN9708. MLN2238 has an improved pharmacodynamic profile and antitumor activity compared with bortezomib in both OCI-Ly10 and PHTX22L models. Although both MLN2238 and bortezomib prolonged overall survival, reduced splenomegaly, and attenuated IgG2a levels in the iMyc(Cα)/Bcl-X(L) GEM model, only MLN2238 alleviated osteolytic bone disease in the DP54-Luc model. The antitumor activity of MLN2238 in a variety of mouse models of B-cell lymphoma and PCM, supporting its clinical development. MLN9708 is being evaluated in multiple phase I and I/II trials.|
|Related CAS||1239908-20-3 (citrate)|
|Synonyms||(R)-(1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutyl)boronic acid; MLN2238; MLN-2238; MLN 2238; Ixazomib Trade name: Ninlaro|
|Current Developer||Millennium Pharmaceuticals, Inc|
PI-1840 potently inhibits proteasomal CT-L activity with IC50 of 0.37 μM in intact human MDA-MB-468 cancer cells, and inhibits proliferation/survival of human M...
RA190, a bis-benzylidine piperidon, is a novel potent and selective inhibitor of proteasome ubiquitin receptor RPN13/ADRM1. RA190 stabilized targets of human pa...
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 pr...
VR23 is a potent and selective inhibitor of trypsin-like proteasomes (IC50 = 1 nmol/L), chymotrypsin-like proteasomes (IC50 = 50-100 nmol/L), and caspase-like p...
Cysteine Protease inhibitor
Cysteine Protease inhibitor is a inhibitor of cysteine protease.
ONX 0914 is an immunoproteasome inhibitor with potential treatment applications in autoimmune disorders, such as rheumatoid arthritis, inflammatory bowel diseas...
MLN-2238 is the biologically active form of MLN9708. MLN2238 has an improved pharmacodynamic profile and antitumor activity compared with bortezomib in both OCI...
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...
The citrate salt form of Ixazomib which is a proteasome inhibitor. It is considered a rollover Phase II trial against multiple myeloma, amyloidosis and lymphoma...
Bortezomib (PS-341) is a potent 20S proteasome inhibitor with Ki of 0.6 nM.
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-101, also known as Calpain Inhibitor I and ALLN, is a calpain inhibitor (IC50 = 0.09 μM) that activates p53-dependent apoptosis in tumor cell lines. Activiti...
PMSF is an irreversible serine/cysteine protease inhibitor.
MG-132 is a potent Proteasome inhibitor with potential anticancer activity. MG-132 induces MCPIP1 expression; induces C6 glioma cell apoptosis via oxidative str...
Oprozomibm, also known as ONX 0912 and PR 047, is an orally bioavailable proteasome inhibitor with potential antineoplastic activity. ONX 0912 inhibits the act...
PD 151746 is a selective, cell-permeable calpain inhibitor with Ki of 0.26 μM for μ-Calpain, about 20-fold selectivity over m-calpain.
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...
AM 114 is an inhibitor of chymotrypsin-like activity of the 20S proteasome. In addition, AM-114 shows anticancer activity, It can inhibit cell growth in human c...