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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.
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.
M14520 PD 151746 PD151746 is a calpain inhibitor, shows a 20-fold selectivity for u-calpain (Ki = 0.26 ± 0.03 μM) over m-calpain (Ki = 5.33 ± 0.77 μM).
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.
M5221 MG-101 MG-101 is a potent inhibitor of cysteine proteases including calpain I (Ki = 190 nM), calpain II (Ki = 220 nM), cathepsin B (Ki = 150 nM), and cathepsin L (Ki = 500 pM). IC50 value: 150 nM (Ki)
M4985 VR23 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 = 3 μM).
M3657 Pepstatin A(Pepstatin) Pepstatin A(Pepstatin) is A specific inhibitor of aspartic proteases produced by actinomycetes, which can inhibit hemoglobin-pepsin, hemoglobin-proctase, Activity of casein-Pepsin, Casein-proctase, Casein-acid protease and hemoglobin, IC50 values are 4.5 nM, 6.2 nM, 150 nM, 290 nM, respectively. 520 nM and 260 nM; At the same time, it can inhibit the activity of HIV protease.
M3478 Gabexate Mesylate Gabexate Mesylate is a serine protease inhibitor with IC50 of 0.19 μM which is used therapeutically in the treatment of pancreatitis and disseminated intravascular coagulation.



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