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Proteasome Proteasome

Inhibitors

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 Bortezomib (PS-341) is a highly selective proteasome inhibitor with a ki value of 6nM.
M7934 MDL 28170 Mdl-28170 (Calpain Inhibitor III) is a potent, selective, membrane-permeable Inhibitor of cysteine protease (Calpain Inhibitor III) that can quickly cross the blood-brain barrier after systemic administration. Mdl-28170 also blocks gamma-secretase.
M2952 PMSF PMSF is an irreversible serine/cysteine protease inhibitor.
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).
M20398 Ixazomib Citrate (MLN9708) Ixazomib Citrate (MLN9708) immediately hydrolyzed to MLN2238, the biologically active form, on exposure to aqueous solutions or plasma. MLN2238 inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50/Ki of 3.4 nM/0.93 nM in cell-free assays, less potent to β1 and little activity to β2. Phase 3.
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.
M14519 ONX-0914 TFA ONX-0914 (PR-957) TFA is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome.
M14518 Marizomib Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, pan-proteasome inhibitor.
M14517 Capzimin Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor.
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.
M13366 (R)-MG-132 (R)-MG-132 (Z-LEu-LEu-Al) is a cellular permeable proteasome and Calpain inhibitor with IC50 of 100 nM and 1.2 μM, respectively.
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.
M11402 TCH-165 Tch-165 is a small molecule modulator of proteasome assembly that increases 20S levels and promotes 20S-mediated protein degradation.
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.
M9577 RA190 hydrochloride RA190 HCl is a potent RPN13 and ADRM1 Inhibitor, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.
M9570 PTP1B-IN-9 PTP1B-IN-9 is a ubiquitin-proteasome system (UPS)-stressor with anticancer activity.
M7934 MDL 28170 Mdl-28170 (Calpain Inhibitor III) is a potent, selective, membrane-permeable Inhibitor of cysteine protease (Calpain Inhibitor III) that can quickly cross the blood-brain barrier after systemic administration. Mdl-28170 also blocks gamma-secretase.
M5966 Sivelestat sodium tetrahydrate Sivelestat sodium tetrahydrate is a competitive inhibitor of human neutrophil elastase, also inhibits leukocyte elastase obtained from rabbit, rat, hamster and mouse.



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