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.

Proteasome Related Products (34):

Cat. No. Product Name Effect Purity
  • HY-13259
    MG-132 Inhibitor >98.0%
    MG-132 is a peptide aldehyde and a potent, reversible, and cell-permeable proteasome inhibitor with an IC50 of 100 nM, and effectively blocks the proteolytic activity of the 26S proteasome complex.
  • HY-10227
    Bortezomib Inhibitor 99.97%
    Bortezomib (PS-341) is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib (PS-341) disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib (PS-341) is an anti-cancer drug and the first therapeutic proteasome inhibitor to be used in humans.
  • HY-10455
    Carfilzomib Inhibitor 99.96%
    Carfilzomib is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.
  • HY-13067
    Tripterin Inhibitor 99.91%
    Tripterin (Celastrol) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM.
  • HY-13207
    ONX-0914 Inhibitor 98.86%
    ONX-0914 (PR-957) is a potent and selective inhibitor of immunoproteasome subunit LMP7.
  • HY-N0375
    18α-Glycyrrhetinic acid Activator 99.19%
    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.
  • HY-N2306A
    Aclacinomycin A hydrochloride Inhibitor 98.08%
    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. Aclacinomycin A hydrochloride is also a dual inhibitor of topoisomerase I and II. An effective anthracycline chemotherapeutic agent for hematologic cancers and solid tumors.
  • HY-100223
    Calpeptin Inhibitor >98.0%
    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.
  • HY-10453
    Ixazomib Inhibitor 99.24%
    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).
  • HY-P0018A
    Pepstatin Trifluoroacetate Inhibitor 99.11%
    Pepstatin 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. Pepstatin Ammonium also inhibits HIV protease.
  • HY-13821
    Epoxomicin Inhibitor 99.89%
    Epoxomicin is a cell-permeable and irreversible proteasome inhibitor, primarily the chymotrypsin-like activity.
  • HY-10452
    Ixazomib citrate Inhibitor >98.0%
    Ixazomib citrate (MLN9708) is a reversible inhibitor of the chymotrypsin-like proteolytic β5 site of the 20S proteasome with an IC50 of 3.4 nM and a Ki of 0.93 nM.
  • HY-100529
    PD150606 Inhibitor >98.0%
    PD 150606 is a selective, cell-permeable non-peptide calpain inhibitor with Ki values of 0.21 μM and 0.37 μM for μ- and m-calpains respectively, which is neuroprotective.
  • HY-18964
    MG-101 Inhibitor
    MG-101 is a potent inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively.
  • HY-P0018
    Pepstatin Inhibitor >98.0%
    Pepstatin 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. Pepstatin Ammonium also inhibits HIV protease.
  • HY-12113
    Oprozomib Inhibitor 99.60%
    Oprozomib (ONX 0912; PR047) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM.
  • HY-100739
    RA190 Inhibitor 98.03%
    RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.
  • HY-110404
    Capzimin Inhibitor 99.19%
    Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor.
  • HY-10454
    Delanzomib Inhibitor >98.0%
    Delanzomib(CEP-18770) is a novel orally-active inhibitor of the chymotrypsin-like activity of the proteasome that down-modulates the nuclear factor-kappaB (NF-kappaB) activity.
  • HY-18236
    MDL-28170 Inhibitor >99.0%
    MDL-28170 (Calpain Inhibitor III) is a potent, selective and membrane-permeable cysteine protease inhibitor of calpain that rapidly penetrates the blood-brain barrier following systemic administration. MDL-28170 also block γ-secretase.
Isoform Specific Products

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