2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Proteasome

Proteasome

Proteasome

Related Products

PDF 1.03 MB

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-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-181499
    RA190-PEG1-NH2
    RA190-PEG1-NH2 (Compound S16), RA190 (HY-100739) derivative, is a Proteasome ligand. RA190-PEG1-NH2 can be used to synthesis FKBP12 CAP-TAC degrader RAFKBP12 (HY-181498).
    RA190-PEG1-NH2
  • 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-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-118522
    TP-110
    		Inhibitor
    TP-110 is a proteasome inhibitor. TP-110 specifically inhibits the protease-like activity of the 20S proteasome, but does not affect the trypsin-like or peptidyl-glutamyl peptide hydrolysis activity. TP-110 inhibits the NF-κB pathway, activates caspase-8, -9, and -3, and causes PARP cleavage, significantly reducing the levels of cIAP-1 and XIAP. TP-110 causes cell cycle arrest at the G2/M phase and promotes apoptosis of cancer cells. TP-110 can be used in cancer research of prostate cancer and multiple myeloma, etc.
    TP-110
  • 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-W720448
    VR23-d8
    VR23-d8 is the deuterium labeled VR23 (HY-18741). VR23 is a small molecule that potently inhibits the activities of trypsin-like proteasomes (IC50=1 nM), chymotrypsin-like proteasomes (IC50=50-100 nM), and caspase-like proteasomes (IC50=3 μM).
    VR23-d<sub>8</sub>
  • HY-159808
    TCL1
    		Inhibitor
    TCL1 is a selective non-covalent inhibitor targeting the Pru domain of the Rpn-13 subunit in the 19S regulatory particle (19S RP) of the proteasome with an IC50 value of approximately 26 μM. TCL1 interferes with the recognition and transport of ubiquitinated proteins by Rpn-13, inhibits the degradation of proteins by the proteasome, and thus affects the balance of intracellular protein metabolism. TCL1 is promising for research of hematological malignancies.
    TCL1
  • 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
  • HY-181940
    Berberine-amide-m-PhBA chloride
    		Inhibitor
    Berberine-amide-m-PhBA chloride (Compound 8b) is a selective anti-breast cancer agent. Berberine-amide-m-PhBA chloride may inhibit the proteasome by interacting with the 20S proteasome β5 subunit. Berberine-amide-m-PhBA chloride can be used in the research of breast cancer.
    Berberine-amide-m-PhBA chloride
  • HY-13067G
    Celastrol (GMP)
    		Inhibitor
    Celastrol (GMP) (Tripterine (GMP)) is Celastrol (HY-10227) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Celastrol (Tripterine;Tripterin) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. In addition, Celastrol is also an antibiotic with potent antimicrobial activity against standard and clinical methicillin-resistant Staphylococcus aureus (MRSA) strains, inducing oxidative stress and inhibiting DNA synthesis by binding to P5CDH.
    Celastrol (GMP)
  • HY-P5379
    Calpastatin subdomain B
    Calpastatin subdomain B is a biological active peptide. (inhibit calpain activity)
    Calpastatin subdomain B
  • HY-N13917
    Argyrin B
    		Inhibitor
    Argyrin B, a natural product cyclic peptide, is a reversible, non-competitive immunoproteasome inhibitor. Argyrin B shows selective inhibition of the β5i and β1i sites of the immunoproteasome over the β5c and β1c sites of the constitutive proteasome with nearly 20-fold selective inhibition of β1i over the homologous β1c. Argyrin B has antibacterial effects.
    Argyrin B
Cat. No. Product Name / Synonyms Application Reactivity