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-N2306A
    Aclacinomycin A hydrochloride
    		Inhibitor
    Aclacinomycin A (Aclarubicin) hydrochloride is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A hydrochloride is an inhibitor of topoisomerase I and II. Aclacinomycin A hydrochloride inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A hydrochloride might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis.
    Aclacinomycin A hydrochloride
  • HY-136563
    RA375
    		Inhibitor 99.31%
    RA375 is a RPN13 (26S proteasome regulatory subunit) inhibitor. RA375 activates UPR signaling, ROS production and apoptosis. RA375 exhibits ten-fold greater activity against cancer lines than RA190, reflecting its nitro ring substituents and the addition of a chloroacetamide warhead.
    RA375
  • HY-P1081
    Acetyl-Calpastatin(184-210)(human)
    		Inhibitor 98.20%
    Acetyl-Calpastatin(184-210)(human) 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)
  • HY-160289
    ARI-3144
    		Inhibitor 99.72%
    ARI-3144 is an excellent substrate for fibroblast activation protein (FAP). ARI-3144 is a FAP-activated proteasome inhibitor that can be used for the research of solid tumors.
    ARI-3144
  • HY-123587
    PR-924
    		Inhibitor 99.34%
    PR-924 is a selective tripeptide epoxyketone immunoproteasome subunit LMP-7 inhibitor with an IC50 of 22 nM. PR-924 covalently modifies proteasomal N-terminal threonine active sites. PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities.
    PR-924
  • HY-136750
    Z-LLY-FMK
    		Inhibitor 98.65%
    Z-LLY-FMK (Calpain Inhibitor IV) is a calpain inhibitor, involved in apoptosis of many cell systems. Z-LLY-FMK inhibits the intestine apoptosis after common bile duct ligation.
    Z-LLY-FMK
  • HY-107412
    Proteasome inhibitor IX
    		Inhibitor 99.43%
    Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC50 value of ~1 μM. Proteasome inhibitor IX exhibits HCT116 p53+/+ cells growth inhibitory activity with an IC50 value of 1.49 μM. Proteasome inhibitor IX has potent anticancer activity.
    Proteasome inhibitor IX
  • HY-134961
    Z-Ala-Arg-Arg-AMC
    		98.00%
    Z-Ala-Arg-Arg-AMC (Fluorogenic Proteasome Substrate) is a fluorogenic substrate for assaying trypsin-like activity of proteasome.
    Z-Ala-Arg-Arg-AMC
  • HY-157034
    LU-002i
    		Inhibitor 99.76%
    LU-002i is a subunit-selective human proteasome β2c and β2i inhibitor with an IC50 value of 220 nM for β2i.
    LU-002i
  • HY-P1259A
    PR-39 TFA
    		Inhibitor 99.96%
    PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice.
    PR-39 TFA
  • HY-D1705
    Ac-ANW-AMC
    		99.40%
    Ac-ANW-AMC is a fluorogenic substrate for immunoproteasome. Ac-ANW-AMC can be used to measure β5i activity (Ex=345 nm, Em=445 nm).
    Ac-ANW-AMC
  • HY-13207A
    ONX-0914 TFA
    		Inhibitor 98.01%
    ONX-0914 (PR-957) TFA is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 TFA blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 TFA is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (Ki=5.2 μM). ONX-0914 TFA reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1.
    ONX-0914 TFA
  • HY-127102
    GSK3494245
    		Inhibitor 98.56%
    GSK3494245 (DDD01305143) is a potent, orally active, and selective inhibitor of the chymotrypsin-like activity of the parasite proteasome binding in a site sandwiched between the β4 and β5 subunits (IC50=0.16 μM for WT L. donovani proteasomes). GSK3494245 moderately inhibits chymotrypsin-like activity of human proteasome (IC50: purified 26S=13 µM; enriched THP-1 extracts IC50=40µM). GSK3494245 exhibits attractive biological and biosafety properties.
    GSK3494245
  • HY-10455S
    Carfilzomib-d8
    		Inhibitor 98.93%
    Carfilzomib-d8 is deuterium labeled Carfilzomib. Carfilzomib (PR-171) is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.
    Carfilzomib-d<sub>8</sub>
  • HY-120234
    Z-LLNle-CHO
    		Inhibitor
    Z-LLNle-CHO (Z-Leu-Leu-Nle-CHO) is a γ-secretase inhibitor I. Z-LLNle-CHO induces caspase and ROS-dependent apoptosis by blocking the Akt-mediated pro-survival pathway. Z-LLNle-CHO can be used in cancer research, such as breast cancer and leukaemia.
    Z-LLNle-CHO
  • HY-144452
    Immunoproteasome inhibitor 1
    		Inhibitor 99.59%
    Immunoproteasome inhibitor 1 is a potent, reversible, time-independent immunoproteasome and proteasome inhibitor (Kis of 1.18, 0.27, 1.91 μM in β5c, β1i, β5i submits, respectively). Immunoproteasome inhibitor 1 can be used for the research of certain neoplastic diseases.
    Immunoproteasome inhibitor 1
  • HY-W001023
    5-Amino-8-hydroxyquinoline
    5-Amino-8-hydroxyquinoline (5A8HQ), a potential anticancer candidate, has promising proteasome inhibitory activity.
    5-Amino-8-hydroxyquinoline
  • HY-135396
    (1S,2S)-Bortezomib
    		Inhibitor
    (1S,2S)-Bortezomib is an enantiomer of Bortezomib. Bortezomib is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki of 0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is an anti-cancer agent and the first therapeutic proteasome inhibitor to be used in humans.
    (1S,2S)-Bortezomib
  • HY-119037
    UK-101
    		Inhibitor 99.58%
    UK-101 is a potent and selective immunoproteasome β1i (LMP2) inhibitor with an IC50 value of 104 nM, displays 144- and 10-fold selectivity over β1c (IC50=15 μM) and β5 subunit (IC50=1 μM), respectivey. UK-101 induces cell apoptosis and can be used for the study of prostate cancer.
    UK-101
  • HY-118933
    Calpain Inhibitor VI
    		Inhibitor
    Calpain Inhibitor VI (SJA6017) is a synthesized peptide aldehyde inhibitor of calpain. Calpain Inhibitor VI inhibits purified m-calpain with the IC50 of 80 nM. Calpain Inhibitor VI can be used for the research of cataract.
    Calpain Inhibitor VI
Cat. No. Product Name / Synonyms Application Reactivity