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-119378
    AK 295
    		Inhibitor
    AK 295 (CX 295) is a calpain inhibitor that inhibits apoptosis through a calpain-dependent pathway. AK 295 improves neurological function in a rat model of spinal cord injury (SCI). AK 295 can be used in the study of neurodegenerative diseases, such as bulbar amyotrophy, stroke, Alzheimer's disease, Parkinson's disease, multiple sclerosis.
    AK 295
  • HY-12743
    K-7174
    		Inhibitor 98.02%
    K-7174 is an orally active proteasome and GATA inhibitor. K-7174 is a cell adhesion inhibitor. K-7174 induces cell apoptosis. K-7174 shows antitumor activities, it can be used for the research of cancer.
    K-7174
  • HY-114419
    Zetomipzomib
    		Inhibitor
    Zetomipzomib (KZR-616), a first-in-class inhibitor of the immunoproteasome, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. Zetomipzomib has the potential for the research of multiple autoimmune diseases.
    Zetomipzomib
  • HY-P10002
    EWFW-ACC
    EWFW-ACC is the tetrapeptide substrate for the immunoproteasome and has selectivity for the LMP7 subunits.
    EWFW-ACC
  • 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.
    Thrombin inhibitor 5
  • HY-116171
    (Rac)-Calpain Inhibitor XII
    		Inhibitor 99.04%
    (Rac)-Calpain Inhibitor XII is a reversible and selective inhibitor of calpain I (μ-calpain, Ki=19 nM). (Rac)-Calpain Inhibitor XII has lower affinities for calpain II (m-calpain, Ki=120 nM) and cathepsin B (Ki=750 nM). (Rac)-Calpain Inhibitor XII has the potential for studying the role of calpains in diverse processes, including neutrophil chemotaxis, neuronal signaling, and cardiac response to injury.
    (Rac)-Calpain Inhibitor XII
  • HY-10227S
    Bortezomib-d8
    		Inhibitor ≥98.0%
    Bortezomib-d8 is the deuterium labeled Bortezomib. 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[1][2].
    Bortezomib-d<sub>8</sub>
  • HY-119288
    BC-23
    		Inhibitor
    BC-23 (NSC 45382) is a proteasome inhibitor. BC-23 exhibits good inhibition of CT-L activity of the proteasome and is selective for malignant over normal cells.
    BC-23
  • HY-109001A
    (1S,2R)-Alicapistat
    		Inhibitor ≥98.0%
    (1S,2R)-Alicapistat ((1S,2R)-ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD). (1S,2R)-Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC50 value of 395 nM.
    (1S,2R)-Alicapistat
  • HY-150226
    Enzyme-IN-1
    		Inhibitor
    Enzyme-IN-1 (compound 1) is a peptide-based inhibitor of N-terminal nucleophile (Ntn) hydrolases. Specifically, Enzyme-IN-1 inhibits the chymotrypsin-like activity (CT-L) of the 20S proteasome. Enzyme-IN-1 may has potential antiinflammatory properties.
    Enzyme-IN-1
  • HY-139331
    20S Proteasome-IN-1
    		Inhibitor 99.13%
    20S Proteasome-IN-1 is a 26S proteasome inhibitor extracted from patent WO2006128196A2 compound 2. 20S Proteasome-IN-1 has the potential for cancer, immune-related disorders, inflammation, ischemic conditions, neurodegenerative disorders and other diseases research.
    20S Proteasome-IN-1
  • HY-112908
    RTS-V5
    		Inhibitor
    RTS-V5 is a dual HDAC/proteasome inhibitor with IC50s of 6.9, 18, 15, 0.27, 0.53 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively.
    RTS-V5
  • HY-150590
    20S Proteasome-IN-2
    		Inhibitor
    20S Proteasome-IN-2 is a human 20S proteasome inhibitor. 20S Proteasome-IN-2 shows high selectivity to its β5 subunit with the IC50 of 0.18 μM. 20S Proteasome-IN-2 displays anti-proliferative effect in vitro and in vivo, and arrests cell cycle at G2/M.
    20S Proteasome-IN-2
  • HY-P4910
    Baceridin
    		Inhibitor
    Baceridin is a proteasome inhibitor and a cyclic hexapeptide. Baceridin can be isolated from the culture medium of Epiphytic Bacillus. Baceridin can inhibit cell cycle progression and induce tumor cell apoptosis through a p53-independent pathway. Baceridin can be used in cancer research.
    Baceridin
  • HY-P4580
    Suc-Ala-Ala-Pro-Phe-SBzl
    Suc-Ala-Ala-Pro-Phe-SBzl can be used as the substrate of rat intestinal mast cell protease (RMCP I), rat skeletal muscle mast cell protease (RMCP II) and Chymotrypsin (HY-108910). Suc-Ala-Ala-Pro-Phe-SBzl can be hydrolyzed by glycine (R208G).
    Suc-Ala-Ala-Pro-Phe-SBzl
  • HY-N11620
    Sadopeptins A
    		Inhibitor
    Sadopeptins A is a nature product that could be isolated from Streptomyces sp. Sadopeptins A is a potent proteasome inhibitor.
    Sadopeptins A
  • HY-162965
    Immunoproteasome activator 1
    		Activator
    Immunoproteasome activator 1 (compound A) is a selective immunoproteasome activator that increases the presentation of individual MHC-I–bound peptides by over 100-fold. Immunoproteasome activator 1 binds to the proteasome structural subunit PSMA1 and promotes the association of the proteasome activator PA28α/β (PSME1/PSME2) with immunoproteasomes.
    Immunoproteasome activator 1
  • HY-158197
    RC-106
    		Inhibitor
    RC-106 is a proteasome inhibitor (IC50: 35 μM) and Sigma receptor modulator with anticancer activity. RC-106 has antiproliferative activity against cancer cells including glioblastoma (GB) and multiple myeloma (MM).
    RC-106
  • HY-142920
    LMP7-IN-1
    		Inhibitor
    LMP7-IN-1, a Boronic acid derivative, is a potent and selective immunoproteasome subunit LMP7 (β5i) inhibitor with an IC50 of 1.83 nM (WO2021143923A1; compound 20).
    LMP7-IN-1
  • HY-P4293
    Z-Leu-Tyr-Chloromethylketone
    Z-Leu-Tyr-Chloromethylketone is a calpain inhibitor.
    Z-Leu-Tyr-Chloromethylketone
Cat. No. Product Name / Synonyms Application Reactivity