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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-N2306R
    Aclacinomycin A (Standard)
    Inhibitor
    Aclacinomycin A (Standard) is the analytical standard of Aclacinomycin A. This product is intended for research and analytical applications. Aclacinomycin A (Aclarubicin) is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A is an inhibitor of topoisomerase I and II. Aclacinomycin A inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis.
    Aclacinomycin A (Standard)
  • HY-N10332
    Leptosphaerodione
    Inhibitor
    Leptosphaerodione, isolated from Remotididymella sp. Fungus, is a potent ubiquitin-proteasome system (UPS) inhibitor. Leptosphaerodione exhibits cytotoxicity in HeLa cells with IC50 value of 3.2 μM. Anti-tumor agent.
    Leptosphaerodione
  • HY-N12618
    Crocapeptin C
    Inhibitor
    Crocapeptin C is a cyclic depsipeptide that can be extrated from Melittangium boletus. Crocapeptin C exhibits potent inhibitory activity against chymotrypsin with an IC50 value of 0.5 µM.
    Crocapeptin C
  • HY-100172
    Proteasome-IN-1
    Inhibitor
    Proteasome-IN-1 is a proteasome inhibitor extracted from patent WO 2013142376 A1.
    Proteasome-IN-1
  • HY-126874
    Tyropeptin A-4
    Inhibitor
    Tyropeptin A-4 (TP-101) is a potent proteasome inhibitor with the ability to inhibit mammalian 20S proteasome activity. Tyropeptin A-4 exerts its inhibitory effect by binding to the site responsible for trypsin-like activity. Tyropeptin A-4 derivative TP-104 has a 20-fold increase in inhibitory activity over Tyropeptin A. TP-110 specifically inhibits trypsin-like activity without affecting PGPH and trypsin-like activity.
    Tyropeptin A-4
  • HY-135070B
    Ac-RLR-AMC TFA
    Ac-RLR-AMC (Ac-Arg-Leu-Arg-AMC) TFA is a fluorogenic substrate for the 26S proteasome (Ex/Em: 380/440-460 nm). AMC is released upon cleavage, and its fluorescence can be used to quantify the trypsin-like activity of 26S proteasomes.
    Ac-RLR-AMC TFA
  • HY-148535
    Calpain Inhibitor XI
    Inhibitor
    Calpain Inhibitor XI is a reversible covalent inhibitor of calpain-1. Calpain Inhibitor XI can be used for the research of neurodegenerative disorders.
    Calpain Inhibitor XI
  • HY-155103
    Antitrypanosomal agent 15
    Inhibitor
    Antitrypanosomal agent 15 (compound 26) is an orally active, brain-penetrant, selective inhibitor against Trypanosoma cruzi proteasome, with an pIC50 of 7.4 and <4 for T. cruzi and human proteasome, respectively. Antitrypanosomal agent 15 has favorable ADME properties and can be used for Chagas disease study.
    Antitrypanosomal agent 15
  • HY-P10169
    Acetyl-Calpastatin(184-210)(human), Negative Control
    Acetyl-Calpastatin(184-210)(human), Negative Control is a control scramble peptide of Acetyl-Calpastatin(184-210)(human) (HY-P1081). Acetyl-Calpastatin(184-210)(human) is a potent, selective and reversible calpain inhibitor.
    Acetyl-Calpastatin(184-210)(human), Negative Control
  • HY-169144
    Bortezomib analog
    Bortezomib analog (Compound 13), an analog of Bortezomib (HY-10227), is an active control of 20S proteasome subunit β5 ligand.
    Bortezomib analog
  • HY-E70525A
    Alpha 2 Macroglobulin, Human Plasma, Fast Form
    Inhibitor
    Alpha 2 Macroglobulin, Human Plasma, Fast Form is a broad-spectrum protease inhibitor, representing the fast form (Fast Form) of Alpha 2 Macroglobulin. Alpha 2 Macroglobulin also has a slow form (Slow Form). The slow form of Alpha 2 Macroglobulin can lure active proteases into its molecular cage and subsequently "tag" its complex for elimination. The fast form of Alpha 2 Macroglobulin is an allosteric product of the slow form, generated when proteases are captured by A2M bait regions, leading to chemical cleavage of internal thioester bonds near the bait regions. Alpha 2 Macroglobulin also promotes cell migration and binds cytokines, growth factors, and damaged extracellular proteins. Alpha 2 Macroglobulin holds research significance in inflammation, immunity, and infection.
    Alpha 2 Macroglobulin, Human Plasma, Fast Form
  • HY-149832
    Anticancer agent 114
    Inhibitor
    Anticancer agent 114 is a potent and orally active dipeptide boronic acid ester proteasome inhibitor with an IC50 value of 2.2 nM. Anticancer agent 114 has antiproliferative activity against the RPMI-8226 cells. Anticancer agent 114 can be used in research of multiple myeloma.
    Anticancer agent 114
  • HY-151195
    20S Proteasome-IN-4
    Inhibitor
    20S Proteasome-IN-4 (Compound 7) is a brain-penetrant, parasite-selective, orally active 20S proteasome inhibitor with an IC50 of 6.3 nM against T. b. brucei 20S proteasome. 20S Proteasome-IN-4 can be used for the research of human African trypanosomiasis (HAT).
    20S Proteasome-IN-4
  • HY-119131
    AK 275
    Inhibitor
    AK 275, a calpain inhibitor, exhibits neuroprotection activity. AK 275 can be used in the study for central nervous system trauma and ischemia.
    AK 275
  • HY-164689
    Cadmium pyrithione
    Inhibitor
    Cadmium pyrithione is a metal compound that inhibits protein deubiquitinase activity. Cadmium pyrithione treatment results in significant accumulation of ubiquitinated proteins in cancer cells and primary leukemia cells. Cadmium pyrithione strongly inhibits the activity of proteasome deubiquitinase (such as USP14 and UCHL5), but has a smaller inhibitory effect on 20S proteasome activity. The anticancer activity of Cadmium pyrithione is associated with the induction of apoptosis through caspase activation. Furthermore, Cadmium pyrithione inhibition inhibited proteasome function and suppressed tumor growth in animal xenograft models.
    Cadmium pyrithione
  • HY-N0375R
    18α-Glycyrrhetinic acid (Standard)
    Activator
    18α-Glycyrrhetinic acid (Standard) is the analytical standard of 18α-Glycyrrhetinic acid. This product is intended for research and analytical applications. 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.
    18α-Glycyrrhetinic acid (Standard)
  • HY-157034A
    LU-002i TFA
    Inhibitor
    LU-002i TFA is a subunit-selective human proteasome β2c and β2i inhibitor with an IC50 value of 220 nM for β2i.
    LU-002i TFA
  • HY-N11621
    Sadopeptins B
    Inhibitor
    Sadopeptins B is a nature product that could be isolated from Streptomyces sp. Sadopeptins B is a potent proteasome inhibitor.
    Sadopeptins B
  • HY-P1081A
    Acetyl-Calpastatin(184-210)(human) TFA
    Inhibitor
    Acetyl-Calpastatin(184-210)(human) TFA is a potent, selective and reversible calpain inhibitor with Ki values of 0.2 nM and 6 μM for µ-calpain and cathepsin L, respectively.
    Acetyl-Calpastatin(184-210)(human) TFA
  • HY-168048
    ZINC09518833
    Inhibitor
    ZINC09518833 is a α-ketoamide nonpeptidic proteasome inhibitor with an IC50 value of 12.4 μM. ZINC09518833 binds both primed and nonprimed sites of the proteasome. ZINC09518833 is promising for research of multiple myeloma (MM).
    ZINC09518833
Cat. No. Product Name / Synonyms Application Reactivity