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

Proteasome

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-126743
    JBIR-22
    Inhibitor
    JBIR-22 is a protein-protein interaction inhibitor of proteasome assembly factor 3 homodimer, which has the activity of inhibiting this interaction and exerting long-term cytotoxicity against human cervical cancer cell lines, and its stereochemical structure has been determined by total synthesis.
    JBIR-22
  • HY-P4348
    MeOSuc-Gly-Leu-Phe-AMC
    MeOSuc-Gly-Leu-Phe-AMC is a peptide substrate of proteasomal.
    MeOSuc-Gly-Leu-Phe-AMC
  • HY-117513
    CEP1612
    Inhibitor
    CEP1612 is a dipeptidyl proteasome inhibitor with the IC50 of 60 nM. CEP1612 induces p21(WAF1)and p27(KIP1) expression and cell apoptosis. CEP1612 shows anticancer activity in vivo.
    CEP1612
  • HY-P1259
    PR-39
    Inhibitor
    PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice.
    PR-39
  • HY-N2117R
    Isoginkgetin (Standard)
    Inhibitor
    Isoginkgetin (Standard) is the analytical standard of Isoginkgetin. This product is intended for research and analytical applications. Isoginkgetin is a pre-mRNA splicing inhibitor inhibitor. Isoginkgetin also inhibits activities of both Akt, NF-κB and MMP-9. Isoginkgetin inhibits the activity of the 20S proteasome, induces apoptosis and activates autophagy.
    Isoginkgetin (Standard)
  • HY-151376
    SAP2-IN-1
    Inhibitor
    SAP2-IN-1 is a secreted aspartic protease 2 (SAP2) inhibitor and has potent SAP2 inhibitory activity with an IC50 value of 0.92 μM. SAP2-IN-1 also is a virulence factor inhibitor and is inactive in vitro. SAP2-IN-1 can be used for the research of infection.
    SAP2-IN-1
  • HY-P10050
    Calpain substrate
    Substrate
    Calpain substrate is the membrane non-permeable fluorogenic calpain substrate and can be used in Calpain enzymatic activity assay.
    Calpain substrate
  • HY-162754
    LMP7/LMP2-IN-1
    Inhibitor
    LMP7/LMP2-IN-1 (Compound 19) is the orally active inhibitor for immunoproteasome subunits LMP7 and LMP2 with IC50 of 257 and 10 nM. LMP7/LMP2-IN-1 reduces the generation of antibody, downregulates the cells in spleen germinal center B and in plasma in NP-OVA-immunized mice, and can be used in research about autoimmune diseases.
    LMP7/LMP2-IN-1
  • HY-113221R
    Isovalerylcarnitine (Standard)
    Activator
    Isovalerylcarnitine (Standard) is the analytical standard of Isovalerylcarnitine. This product is intended for research and analytical applications. Isovalerylcarnitine is a product of the catabolism of L-leucine. Isovalerylcarnitine is also a selective and reversible calpain activator that induces apoptosis.
    Isovalerylcarnitine (Standard)
  • HY-N14928
    Phepropeptin B
    Inhibitor
    Phepropeptin B, a microbial secondary metabolite, is a proteasome inhibitor with an IC50 of 11 μg/mL.
    Phepropeptin B
  • HY-W409181
    (Rac)-PD 151746
    Inhibitor
    (Rac)-PD 151746 is the optically inactive racemate of PD 151746 (HY-19749). PD 151746 is a neuroprotective calpain inhibitor with Ki values of 0.26 μM (u-calpain) and 5.33 μM (m-calpain), respectively.
    (Rac)-PD 151746
  • HY-N2306R
    Aclacinomycin A (Standard)
    Inhibitor
    Aclacinomycin A (Standard) is the analytical standard of Aclacinomycin A. This product is intended for research and analytical applications. 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 (Standard)
  • 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-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-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-W048404
    Bortezomib impurity A
    Control
    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-129867
    Z-Leu-Leu-Leu-AMC
    Z-Leu-Leu-Leu-AMC is a fluorogenic substrate for measuring the chymotrypsin-like protease activity of the 20S proteasome.
    Z-Leu-Leu-Leu-AMC
Cat. No. Product Name / Synonyms Application Reactivity