2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Proteasome

Proteasome

Proteasome

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Proteasomes are very large protein complexes inside all eukaryotes and archaea, and in some bacteria. In eukaryotes, they are located in the nucleus and the cytoplasm. The main function of the proteasome is to degrade unneeded or damaged proteins by proteolysis, a chemical reaction that breaks peptide bonds. Enzymes that carry out such reactions are called proteases. Proteasomes are part of a major mechanism by which cells regulate the concentration of particular proteins and degrade misfolded proteins. The degradation process yields peptides of about seven to eight amino acids long, which can then be further degraded into amino acids and used in synthesizing new proteins. Proteins are tagged for degradation with a small protein called ubiquitin. The tagging reaction is catalyzed by enzymes called ubiquitin ligases. Once a protein is tagged with a single ubiquitin molecule, this is a signal to other ligases to attach additional ubiquitin molecules. The result is a polyubiquitin chain that is bound by the proteasome, allowing it to degrade the tagged protein.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-12113
    Oprozomib
    		Inhibitor 99.76%
    Oprozomib (PR-047) is an orally bioavailable and selective peptide epoxyketone proteasome inhibitor with IC50s of 36 and 82 nM for proteasome (β5) and immunoproteasome (LMP7), respectively. Oprozomib (ONX 0912) induces apoptosis in MM cells.
    Oprozomib
  • HY-N2306
    Aclacinomycin A
    		Inhibitor 99.30%
    Aclacinomycin A (Aclarubicin) is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A is an inhibitor of topoisomerase I and II. Aclacinomycin A inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis.
    Aclacinomycin A
  • HY-13259D
    MG-132 (negative control)
    		Control ≥98.0%
    MG-132 negative control is the negative control form of MG-132 (HY-13259). MG-132 is a potent proteasome and calpain inhibitor.
    MG-132 (negative control)
  • HY-N0375
    18α-Glycyrrhetinic acid
    		Activator 99.52%
    18α-Glycyrrhetinic acid, a diet-derived compound, is an inhibitor of NF-kB and an activator of proteasome, which serves as pro-longevity and anti-aggregation factor in a multicellular organism. 18α-Glycyrrhetinic acid induces apoptosis.
    18α-Glycyrrhetinic acid
  • HY-10454
    Delanzomib
    		Inhibitor ≥98.0%
    Delanzomib (CEP-18770) is a potent and orally active chymotrypsin-like activity of the proteasome inhibitor with an IC50 of 3.8 nM. Delanzomib inhibits NF-κB activity, induces cancer cell apoptotic, and has strong antiangiogenic and anti-cancer activities.
    Delanzomib
  • HY-12743A
    K-7174 dihydrochloride
    		Inhibitor 98.60%
    K-7174 dihydrochloride is an orally active proteasome and GATA inhibitor. K-7174 dihydrochloride is a cell adhesion inhibitor. K-7174 dihydrochloride induces cell apoptosis. K-7174 dihydrochloride shows antitumor activities, it can be used for the research of cancer.
    K-7174 dihydrochloride
  • HY-N2166
    Tomatine
    		Inhibitor 99.90%
    Tomatine is a glycoalkaloid, found in the tomato plant (Lycopersicon esculentum Mill.). 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.
    Tomatine
  • HY-151424
    Vimentin-IN-1
    		99.64%
    Vimentin-IN-1 is a FiVe1 derivative, an orally active and selective anticancer agent. FiVe1 binds type III intermediate filament protein vimentin (VIM), to induce hyperphosphorylation of Ser56, resulting selective disruption of mitosis and multinucleation in transformed VIM-expressing mesenchymal cancer cells. Vimentin-IN-1 shows better oral bioavailability and pharmacokinetic profiles than FiVe1.
    Vimentin-IN-1
  • HY-120722
    TCH-165
    		Modulator 99.32%
    TCH-165 is a small molecule modulator of proteasome assembly, which increases 20S levels and facilitates 20S-mediated protein degradation.
    TCH-165
  • HY-153034
    LONP1-IN-2
    		Inhibitor 99.74%
    LONP1-IN-2 (compound 9e) is a potent and selective LONP1 inhibitor with IC50 values of 0.093 μM and >10 μM for LONP1 and 20S proteasome, respectively. LONP1-IN-2 can be used in research of cancer.
    LONP1-IN-2
  • HY-114419A
    Zetomipzomib maleate
    		Inhibitor 99.84%
    Zetomipzomib (KZR-616) maleate, a first-in-class immunoproteasome inhibitor, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP2/mLMP2) subunits of the immunoproteasome. Zetomipzomib maleate has the potential for the research of multiple autoimmune diseases.
    Zetomipzomib maleate
  • HY-E70005H
    Collagenase, Type VIII
    Collagenase, Type VIII is a mixed enzyme derived from Clostridium histolyticum that contains collagenase, a nonspecific protease, and a clostripain. Collagenase, Type VIII can hydrolyze Type VIII collagen and may be used to study the formation of atherosclerosis. Type VIII collagen is a regulator of endothelial cell differentiation and angiogenesis, a substrate for cell adhesion and migration such as smooth muscle cells, and may accumulate in atherosclerosis. After endotoxin activates the expression of Collagenase, Type VIII, it can reduce the production of Type VIII collagen and has the potential to inhibit atherosclerosis.
    Collagenase, Type VIII
  • HY-150602
    20S Proteasome activator 1
    		Activator 99.83%
    20S Proteasome activator 1 is a potent 20S proteasome activator with EC200 values of 0.3 μM, 0.7 μM and 1.8 μM for trypsin-like site, chymotrypsin-like site and caspase-like site. 20S Proteasome activator 1 translates well in a cellular system, preventing the accumulation of the pathogenic A53T mutant of α-synuclein. 20S Proteasome activator 1 can be used for researching neurodegenerative diseases.
    20S Proteasome activator 1
  • HY-111790
    M3258
    		Inhibitor ≥98.0%
    M3258 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 exerts high biochemical (IC50=3.6 nM) and cellular (IC50=3.4 nM) potency against the LMP7 subunit. M3258 shows strong antitumor efficacy in multiple myeloma xenograft models. M3258 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells.
    M3258
  • HY-108552
    MG-115
    		Inhibitor 98.69%
    MG-115 is a potent and reversible proteasome inhibitor, with Kis of 21 nM and 35 nM for 20S and 26S proteasome, respectively. MG-115 specifically inhibit the chymotrypsin-like activity of the proteasome, induces p53-dependent apoptosis.
    MG-115
  • HY-P3414A
    Proteasome-activating peptide 1 TFA
    		Activator 99.82%
    Proteasome-activating peptide 1 TFA is a peptide and a potent proteasome activator. Proteasome-activating peptide 1 TFA increases the chymotrypsin-like proteasomal catalytic activity and, consequently, proteolytic rates both in vitro and in culture. Proteasome-activating peptide 1 TFA prevents protein aggregation in a cellular model of amyotrophic lateral sclerosis.
    Proteasome-activating peptide 1 TFA
  • HY-123053
    Z-Leu-Leu-Glu-AMC
    		99.91%
    Z-Leu-Leu-Glu-AMC is a substrate peptide, and can be used for determination of postacidic-like hydrolysing activity of 20S proteasome
    Z-Leu-Leu-Glu-AMC
  • HY-B0385
    Gabexate mesylate
    		Inhibitor 99.14%
    Gabexate mesylate (FOY) is is a competitive and non-antigenic synthetic inhibitor of trypsin-like serine proteinases. Gabexate mesylate inhibits human thrombin, urokinase, plasmin, and Factor Xa with Kis of 0.97, 1.3, 1.6, and 8.5 μM, respectively. Gabexate mesylate binds to human and bovine tryptase with Kis of 3.4 nM and 18 μM, respectively. Gabexate mesylate exerts an anticoagulant effect on the clotting activity of thrombin and has anti-inflammatory effect by viainhibition of NF-κB, proinflammatory cytokines, and nitric oxide. Gabexate mesylate is used for pancreatitis and disseminated intravascular coagulation.
    Gabexate mesylate
  • HY-100739
    RA190
    		Inhibitor 99.04%
    RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.
    RA190
  • HY-19749
    PD 151746
    		Inhibitor
    PD151746 is a calpain inhibitor, shows a 20-fold selectivity for u-calpain (Ki = 0.
    PD 151746
Cat. No. Product Name / Synonyms Application Reactivity