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-N15130
    Cerpegin
    		Inhibitor
    Cerpegin, a pyridinone-fused c-lactone, is an inhibitor of 20S proteasome. Cerpegin can be used as a tranquillizer, anti-inflammatory, analgesic and antiulcer.
    Cerpegin
  • HY-171956
    Carmaphycin-17
    		Inhibitor
    Carmaphycin-17 (CP-17) is a selective 20S proteasome inhibitor with an EC50 of 217 ?nM. Carmaphycin-17 has potent antimicrobial activity against Trichomonas vaginalis. Carmaphycin-17 overcomes Metronidazole (HY-B0318) resistance and significantly reduces parasite burden upon topical treatment without any apparent adverse effects in vaginal trichomonad infection mice model. Carmaphycin-17 can be used for sexually transmitted disease like trichomoniasis research.
    Carmaphycin-17
  • HY-N14940
    Phepropeptin D
    		Inhibitor
    Phepropeptin D, a microbial secondary metabolite, is a proteasome inhibitor with an IC50 of 7.8 μg/mL.
    Phepropeptin D
  • HY-N6013R
    Aloin (mixture of A&B) (Standard)
    		Inhibitor
    Aloin (mixture of A&B) (Standard) is the analytical standard of Aloin (mixture of A&B) (HY-N6013). This product is intended for research and analytical applications. Aloin (mixture of A&B) is an orally active anthraquinone derivative isolated from Aloe vera. Aloin (mixture of A&B) mitigates airway impairment and exerts neuroprotective, anti-inflammatory, antioxidant, antibacterial, antifungal, antiviral and antitumor effects. Aloin (mixture of A&B) inhibits Clostridium histolyticum collagenase, granulocyte matrix metalloproteinases and human 20S proteasome. Aloin (mixture of A&B) upregulates the Nrf2/HO-1 pathway, suppresses the TGF-β/Smad2/3 pathway. Aloin (mixture of A&B) reduces IL-4/IL-5/IL-13 levels, and reverses oxidative stress markers (MDA, SOD, GSH). Aloin (mixture of A&B) can be used for research on chronic ulcers, burns, wounds, inflammatory and degenerative disorders, asthma and neuroblastoma.
    Aloin (mixture of A&B) (Standard)
  • HY-10453R
    Ixazomib (Standard)
    		Inhibitor
    Ixazomib (Standard) is the analytical standard of Ixazomib. This product is intended for research and analytical applications. Ixazomib (MLN2238) is a selective, potent, and reversible proteasome inhibitor, which inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC50 of 3.4 nM (Ki of 0.93 nM).
    Ixazomib (Standard)
  • HY-B0385R
    Gabexate mesylate (Standard)
    		Inhibitor
    Gabexate (mesylate) (Standard) is the analytical standard of Gabexate (mesylate). This product is intended for research and analytical applications. 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 (Standard)
  • HY-129407
    AAF-CMK TFA
    AAF-CMK TFA (Ala-ala-phe-chloromethylketone tfa; N-Ala-Ala-Phe-CMK) is a subtilisin-type serine peptidase that removes tripeptides from the free NH2 termini of oligopeptides. AAF-CMK TFA is an irreversible inhibitor of TPPII and is typically used at concentrations of 10-100 μM. It does not significantly interfere with the chymotrypsin-like activity of the proteasome. AAF-CMK also inhibits bleomycin hydrolase and puromycin-sensitive aminopeptidase when used at a concentration of 50 μM.
    AAF-CMK TFA
  • HY-N7056R
    4'-Hydroxychalcone (Standard)
    		Inhibitor
    4'-Hydroxychalcone (Standard) is the analytical standard of 4'-Hydroxychalcone (HY-N7056). This product is intended for research and analytical applications. 4'-Hydroxychalcone is a chalcone isolated from licorice root, with hepatoprotective activity. 4'-Hydroxychalcone inhibits TNFα-induced NF-κB activation via proteasome inhibition. 4'-Hydroxychalcone induces a rapid potassium release from mitochondrial vesicles and causes deterioration of respiratory control and oxidative phosphorylation of isolated rat liver mitochondria.
    4'-Hydroxychalcone (Standard)
  • HY-N2166R
    Tomatine (Standard)
    		Inhibitor
    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 (Standard)
  • HY-109001R
    Alicapistat (Standard)
    		Inhibitor
    Alicapistat (Standard) is the analytical standard of Alicapistat (HY-109001). This product is intended for research and analytical applications. Alicapistat (ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD). Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC50 value of 395 nM.
    Alicapistat (Standard)
  • HY-W048404
    Bortezomib impurity A
    		Control 99.75%
    Bortezomib impurity A is a metabolite of the 20S proteasome inhibitor Bortezomib (HY-10227).
    Bortezomib impurity A
  • HY-164487
    JBJ-08-178-01
    		Inhibitor
    JBJ-08-178-01 is a mutant-selective tyrosine kinase inhibitor against human epidermal growth factor receptor 2 (HER2) with an antitumoral activity. JBJ-08-178-01 reduces both the kinase activity and protein levels of HER2 by inducing proteasomal degradation of the receptor in lung cancer. JBJ-08-178-01 is promising for research of non-small-cell lung cancer.
    JBJ-08-178-01
  • HY-179273
    Proteasome-IN-8
    		Inhibitor
    Proteasome-IN-1 (Compound 130) is a proteasome inhibitor. Proteasome-IN-1 exhibits antiparasitic activity against P. faciparum 3D7.
    Proteasome-IN-8
  • HY-W748328
    Ixazomib-13C2,15N
    		Inhibitor
    Ixazomib-13C2,15N is 13C and 15N labeled Ixazomib. Ixazomib (MLN2238) is a selective, potent, and reversible proteasome inhibitor, which inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC50 of 3.4 nM (Ki of 0.93 nM).
    Ixazomib-<sup>13</sup>C<sub>2</sub>,<sup>15</sup>N
  • HY-170363
    Proteasome-IN-6
    		Inhibitor
    Proteasome-IN-6 (Compound J-80) inhibits the β5 catalytic subunit of the Trypanosoma brucei 20S proteasome, inibits T. b. brucei, T. b. gambiense and T. b. rhodesiense with EC50s of 157 nM, 220 nM and 156 nM, respectively. Proteasome-IN-6 exhibits antitrypanosomal activity in mouse model.
    Proteasome-IN-6
  • HY-B0914AR
    10-Undecenoic acid zinc salt (Standard)
    		Inhibitor
    10-Undecenoic acid (zinc salt) (Standard) is the analytical standard of 10-Undecenoic acid (zinc salt). This product is intended for research and analytical applications. 10-Undecenoic acid zinc salt (Undecylenic acid zinc salt) is an antifungal agent. 10-Undecenoic acid zinc salt inhibits Aβ oligomerization, scavenges ROS and inhibits μ-calpain activity. 10-Undecenoic acid zinc salt has neuroprotective effects. 10-Undecenoic acid zinc salt has anticancer effects on a variety of tumors. 10-Undecenoic acid zinc salt inhibits C. albicans biofilm formation and MRSA infection. 10-Undecenoic acid zinc salt inhibits quorum sensing signals of Bacillus subtilis and Pseudomonas aeruginosa.
    10-Undecenoic acid zinc salt (Standard)
  • HY-183009
    Pf20S-IN-1
    		Inhibitor
    Pf20S-IN-1 is a selective inhibitor of the 20S proteasome β5 subunit of Plasmodium falciparum. Pf20S-IN-1 exhibits antiparasitic activity against Plasmodium falciparum, with an EC50 of 20.1 nM against the Plasmodium falciparum W2 strain. Pf20S-IN-1 shows weak inhibitory effect on human 20S proteasome, has no obvious toxicity to human foreskin fibroblasts (HFF), and has a selectivity index > 25000. Pf20S-IN-1 can be used in malaria research.
    Pf20S-IN-1
  • HY-107412R
    Proteasome inhibitor IX (Standard)
    		Inhibitor
    Proteasome inhibitor IX (Standard) is the analytical standard of Proteasome inhibitor IX (HY-107412). This product is intended for research and analytical applications. Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC50 value of ~1 μM. Proteasome inhibitor IX exhibits HCT116 p53+/+ cells growth inhibitory activity with an IC50 value of 1.49 μM. Proteasome inhibitor IX has potent anticancer activity.
    Proteasome inhibitor IX (Standard)
  • HY-145542R
    Isovalerylcarnitine chloride (Standard)
    		Activator
    Isovalerylcarnitine chloride (Standard) is the analytical standard of Isovalerylcarnitine chloride (HY-145542). This product is intended for research and analytical applications. Isovalerylcarnitine chloride is a metabolite of leucine. Isovalerylcarnitine can specifically activate calpain in human neutrophils. Isovalerylcarnitine chloride inhibits tumor cell proliferation and induces apoptosis. Elevated circulating levels of Isovalerylcarnitine chloride are negatively correlated with reduced lung cancer risk.
    Isovalerylcarnitine chloride (Standard)
  • HY-100223R
    Calpeptin (Standard)
    		Inhibitor
    Calpeptin (Standard) is the analytical standard of Calpeptin. This product is intended for research and analytical applications. Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID50 of 40 nM for Calpain I in human platelets. Calpeptin is also an inhibitor of cathepsin K.
    Calpeptin (Standard)
Cat. No. Product Name / Synonyms Application Reactivity