| Cat.No. | Name | Information |
|---|---|---|
| M1902 | MG132 | MG132 is a specific and potent cell-permeable proteasome inhibitor (IC50 = 100 nM, Ki = 4 nM). |
| M2071 | ONX-0914 | Onx-0914 (PR-957) is a selective inhibitor of low molecular weight polypeptide 7 (LMP7), a chymotrypsin subunit of the immune proteasome. Onx-0914 blocks cytokine production and reduces the progression of experimental arthritis. Onx-0914 is a non-competitive irreversible inhibitor of mycobacterium proteasome (Ki=5.2 μM). Onx-0914 activates latent HIV-1 through HF-1-mediated p-TEFb activation. |
| M1686 | Bortezomib (PS-341) | Bortezomib (PS-341) is a highly selective proteasome inhibitor with a ki value of 6nM. |
| M2193 | Epoxomicin | Epoxomicin (BU-4061T) is a cell-permeable, selective and irreversible proteasome inhibitor with an IC50 value of 4 nM. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. |
| M2035 | IU1 | IU1 is a reversible, small molecule inhibitor of deubiquitination by USP14 that demonstrates an IC50 value of 4-5 μM. |
| M3884 | Celastrol | Celastrol (Tripterin) is a potent antioxidant and anti-inflammatory agent, as well as a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. |
| M27794 | ALLM | ALLM (Calpain inhibitor II) is a potent inhibitor of calpain and cathepsin proteases. ALLM inhibits neuronal cell death and improves chronic neurological function after spinal cord injury (SCI). |
| M21515 | Zetomipzomib maleate | Zetomipzomib (KZR-616) maleate is a first-in-class inhibitor of immunoproteasome that selectively targets the immunoproteasome subunit LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50:131/179 nM=hLMP7/mLMP7). Potential of Zetomipzomib maleate for use in multiple autoimmune diseases. |
| M21267 | LXE408 | LXE408 is an oral antileishmanarial compound that selectively targets the kinetoplastid proteosome vs. the mammalian proteosome. |
| M21181 | Zetomipzomib | Zetomipzomib (KZR-616) is the first immunoproteasome inhibitor that selectively targets the immunoproteasome subunits LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7). Zetomipzomib has potential for use in a variety of autoimmune diseases. |
| M20599 | PI-1840 | PI-1840 is a reversible and selective chymotrypsin-like (CT-L) inhibitor with IC50 of 27 nM with little effects on the other two major proteasome proteolytic activities, trypsin-like (T-L) and postglutamyl-peptide-hydrolysis-like (PGPH-L). |
| M19378 | Tomatine | Tomatine elicits neurotoxicity in RIP1 kinase and caspase-independent manner. Tomatine promotes the upregulation of nuclear apoptosis inducing factor (AIF) in neuroblastoma cells. Tomatine also inhibits 20S proteasome activity. |
| M14522 | Pepstatin Trifluoroacetate | Pepstatin Trifluoroacetate (Pepstatin A Trifluoroacetate) is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. |
| M14521 | Pepstatin Ammonium | Pepstatin Ammonium is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. |
| M14516 | Aclacinomycin A hydrochloride | Aclacinomycin A hydrochloride (Aclarubicin hydrochloride), a fluorescent molecule and the first described non-peptidic inhibitor showing discrete specificity for the CTRL (chymotrypsin-like) activity of the 20S proteasome. |
| M11459 | ML604440 | ML604440 is a potent, specific and cell-permeable inhibitor of the proteasome β 1I (LMP2) subunit. ML604440 disrupts MHC class I cell surface expression, IL-6 secretion and naive T helper differentiation to 17 T helper cells. ML604440 improves experimental colitis and EAE disease. |
| M11294 | Alicapistat | Alicapistat (ABT-957) is an orally active, selective inhibitor of human calpains 1 and 2 that can be used in alzheimer's disease (AD) studies. |
| M10767 | M-3258 | M3258 is an oral bioavailable, potent, reversible, and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 for LMP7 IC50 is 3.6 nM in cells IC50 3.4 nM. |
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