1. Metabolic Enzyme/Protease
  2. 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 (26):

Cat. No. Product Name Effect Purity
  • HY-13259
    MG-132 Inhibitor >98.0%
    MG-132 is a potent, non-specific 20S proteasome inhibitor, with IC50 of 24.2 nM for the β5 chymotrypsin-like active site.
  • HY-10227
    Bortezomib Inhibitor 99.97%
    Bortezomib is a potent 20S proteasome inhibitor with Ki of 0.6 nM.
  • HY-10455
    Carfilzomib Inhibitor 99.26%
    Carfilzomib is an irreversible proteasome inhibitor with IC50 of < 5 nM in ANBL-6 and RPMI 8226 cells.
  • HY-13067
    Celastrol Inhibitor 99.90%
    Celastrol is a proteasome inhibitor, potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome (IC50=2.5 μM).
  • HY-B0496
    PMSF Inhibitor >99.0%
    PMSF is an irreversible serine/cysteine protease inhibitor.
  • HY-P0018A
    Pepstatin Trifluoroacetate Inhibitor 99.11%
    Pepstatin Trifluoroacetate is a specific aspartic proteases inhibitor produced by actinomycetes, and also inhibits HIV protease. Sequence: Isovaleryl-Val-Val-Sta-Ala-Sta-OH.
  • HY-110404
    Capzimin Inhibitor 99.19%
    Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor.
  • HY-101286
    Rpn11-IN-1 Inhibitor
    Rpn11-IN-1 is a potent and selective inhibitor of proteasome subunit Rpn11 with an IC50 of 390 nM.
  • HY-P0018
    Pepstatin Inhibitor 98.45%
    Pepstatin is a specific aspartic proteases inhibitor produced by actinomycetes, and also inhibits HIV protease. Sequence: Isovaleryl-Val-Val-Sta-Ala-Sta-OH.
  • HY-13821
    Epoxomicin Inhibitor 99.89%
    Epoxomicin(BU-4061T) is a potent anti-tumor agent isolated from Actinomycetes that is used as a selective and irreversible inhibitor of the 20S proteasome.
  • HY-10453
    MLN2238 Inhibitor >98.0%
    MLN2238 is a selective, potent, and reversible proteasome inhibitor, which inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC50 value of 3.4 nM (Ki of 0.93 nM).
  • HY-18964
    MG-101 Inhibitor
    MG-101 is a potent inhibitor of cysteine proteases including calpain I (Ki = 190 nM), calpain II (Ki = 220 nM), cathepsin B (Ki = 150 nM), and cathepsin L (Ki = 500 pM).
  • HY-13207
    ONX-0914 Inhibitor 98.60%
    ONX-0914 (PR-957) is a potent and selective immunoproteasome inhibitor with minimal cross-reactivity for the constitutive proteasome.
  • HY-10452
    MLN9708 Inhibitor >98.0%
    MLN9708 rapidly hydrolyzes to MLN2238, which is a selective, orally bioavailable, second-generation proteasome inhibitor, inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC50 value of 3.4 nM (Ki of 0.93 nM), and also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites with IC50 of 31 and 3500 nM, respectively.
  • 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-100529
    PD150606 Inhibitor >98.0%
    PD 150606 is a selective, cell-permeable non-peptide calpain inhibitor (Ki values for ν and m-calpains are 0.21 and 0.37 μM respectively).
  • HY-10454
    Delanzomib Inhibitor
    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-100739
    RA190 Inhibitor 98.03%
    RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.
  • HY-18741
    VR23 Inhibitor
    VR23 is a small molecule that potently inhibited the activities of trypsin-like proteasomes (IC50 = 1 nM), chymotrypsin-like proteasomes (IC50 = 50-100 nM), and caspase-like proteasomes (IC50 = 3 μM).
  • HY-19749
    PD 151746 Inhibitor 98.21%
    PD151746 is a calpain inhibitor, shows a 20-fold selectivity for u-calpain (Ki = 0.26 ± 0.03 μM) over m-calpain (Ki = 5.33 ± 0.77 μM).
Isoform Specific Products

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