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.

Signaling Pathways

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Proteasome Proteasome

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