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 (96):

Cat. No. Product Name Effect Purity
  • HY-13259
    MG-132
    Inhibitor ≥98.0%
    MG-132 (Z-Leu-Leu-Leu-al) is a potent proteasome and calpain inhibitor with IC50s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, also is an autophagy activator. MG-132 also induces apoptosis.
  • HY-10227
    Bortezomib
    Inhibitor 99.97%
    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.
  • HY-10455
    Carfilzomib
    Inhibitor 99.96%
    Carfilzomib (PR-171) is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.
  • HY-13067
    Tripterin
    Inhibitor 99.90%
    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-13259C
    (R)-MG-132
    Inhibitor ≥98.0%
    (R)-MG-132 ((S,R,S)-(-)-MG-132) is the enantiomer of MG-132. (R)-MG-132 is a proteasome inhibitor with weaker cell cytotoxicity than MG-132. (R)-MG-132 stereoisomer is a more potent proteasome inhibitor than MG-132.
  • HY-P3414A
    Proteasome-activating peptide 1 TFA
    Activator
    Proteasome-activating peptide 1 TFA is a peptide and a potent proteasome activator. Proteasome-activating peptide 1 TFA increases the chymotrypsin-like proteasomal catalytic activity and, consequently, proteolytic rates both in vitro and in culture. Proteasome-activating peptide 1 TFA prevents protein aggregation in a cellular model of amyotrophic lateral sclerosis.
  • HY-W017227
    Alloxan hydrate
    Inhibitor 99.37%
    Alloxan hydrate is a diabetogenic agent to induce diabetes. Alloxan hydrate is a proteasome inhibitor. Alloxan causes diabetes in experimental animals through its ability to destroy the insulin-secreting B-cells of the pancreas.
  • HY-148037
    Thrombin inhibitor 5
    Inhibitor 99.82%
    Thrombin inhibitor 5 (compound 385) is a thrombin inhibitor, with IC50s ranging from 0.1 μM to 1 μM. Thrombin inhibitor 5 can be used for research of venous thromboembolism.
  • HY-P0018
    Pepstatin
    Inhibitor 98.40%
    Pepstatin (Pepstatin A) 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-10453
    Ixazomib
    Inhibitor 99.06%
    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-13821
    Epoxomicin
    Inhibitor 99.11%
    Epoxomicin (BU-4061T) is an epoxyketone-containing natural product and a potent, selective and irreversible proteasome inhibitor. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. Epoxomicin has strongly antitumor and anti-inflammatory activity.
  • 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-13207
    ONX-0914
    Inhibitor 99.72%
    ONX-0914 (PR-957) is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (Ki=5.2 μM). ONX-0914 reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1.
  • HY-N2117
    Isoginkgetin
    Inhibitor 99.73%
    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.
  • HY-100529
    PD150606
    Inhibitor 98.19%
    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 ≥98.0%
    MG-101 (ALLN) is an 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. MG-101 induces apoptosis and inhibits tumor growth, it can be used for the research of colon cancer.
  • HY-10985
    Marizomib
    Inhibitor 99.55%
    Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, pan-proteasome inhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC50=3.5, 28, and 430 nM, respectively).
  • HY-10452
    Ixazomib citrate
    Inhibitor 99.89%
    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-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.
  • HY-N2306A
    Aclacinomycin A hydrochloride
    Inhibitor
    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.