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-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-10227R
    Bortezomib (Standard)
    		Inhibitor
    Bortezomib (Standard) is the analytical standard of Bortezomib. This product is intended for research and analytical applications. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity.
    Bortezomib (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-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
  • HY-N13917
    Argyrin B
    		Inhibitor
    Argyrin B, a natural product cyclic peptide, is a reversible, non-competitive immunoproteasome inhibitor. Argyrin B shows selective inhibition of the β5i and β1i sites of the immunoproteasome over the β5c and β1c sites of the constitutive proteasome with nearly 20-fold selective inhibition of β1i over the homologous β1c. Argyrin B has antibacterial effects.
    Argyrin B
  • 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-W654243
    Isovalerylcarnitine-d9-1 chloride
    		Activator
    Isovalerylcarnitine-d9-1 (chloride) is deuterium labeled Isovalerylcarnitine (chloride). Isovalerylcarnitine chloride, a product of the catabolism of L-leucine, is a potent activator of the Ca2+-dependent proteinase (calpain) of human neutrophils.
    Isovalerylcarnitine-d<sub>9</sub>-1 chloride
  • 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-10455R
    Carfilzomib (Standard)
    		Inhibitor
    Carfilzomib (Standard) is the analytical standard of Carfilzomib. This product is intended for research and analytical applications. Carfilzomib (PR-171) is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.
    Carfilzomib (Standard)
  • HY-N13904
    Argyrin A
    		Inhibitor
    Argyrin A, a cyclical peptide, is a potent antitumoral agent. Argyrin A exerts its effects through a potent inhibition of the proteasome. Argyrin A leads to increased endogenous p27kip1 levels by preventing protein turnover.
    Argyrin A
  • HY-N14927
    Phepropeptin A
    		Inhibitor
    Phepropeptin A, a microbial secondary metabolite, is a proteasome inhibitor with an IC50 of 21 μg/mL.
    Phepropeptin A
Cat. No. Product Name / Synonyms Application Reactivity