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-P2016
    Ac-Nle-Pro-Nle-Asp-AMC
    		98.72%
    Ac-Nle-Pro-Nle-Asp-AMC is a specific substrate for 26S proteasome. Ac-Nle-Pro-Nle-Asp-AMC can be used for the 26S proteasome caspase-like activity analysis.
    Ac-Nle-Pro-Nle-Asp-AMC
  • HY-145155
    Calpain-2-IN-1
    		Inhibitor 98.05%
    Calpain-2-IN-1 (Formula 1A) is a isoform-specific calpain-2 inhibitor with Kis of 181 nM and 7.8 nM for calpain-1, and calpain-2, respectively. Calpain-2-IN-1 can be used for the research of neurodegenerative diseases and other diseases of synaptic function.
    Calpain-2-IN-1
  • HY-145542
    Isovalerylcarnitine chloride
    		Activator 99.48%
    Isovalerylcarnitine chloride is a metabolite of leucine. Isovalerylcarnitine chloride can specifically activate calpain in human neutrophils. Isovalerylcarnitine chloride inhibits tumor cell proliferation and induces apoptosis. Elevated circulating levels of Isovalerylcarnitine chloride are negatively correlated with reduced lung cancer risk.
    Isovalerylcarnitine chloride
  • HY-13067R
    Celastrol (Standard)
    		Inhibitor
    Celastrol (Standard) is the analytical standard of Celastrol. This product is intended for research and analytical applications. 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.
    Celastrol (Standard)
  • HY-109059
    Fulacimstat
    		Inhibitor 99.86%
    Fulacimstat is an orally available chymase inhibitor, with IC50s of 4, 3 nM for human and hamster chymase enzyme, respectively.
    Fulacimstat
  • HY-139066
    Punicic acid
    		Inhibitor 98.5%
    Punicic acid is a bioactive compound of pomegranate seed oil. Punicic acid is an isomer of conjugated α-linolenic acid and ω-5 polyunsaturated fatty acids. Punicic acid has anti-inflammatory and antioxidant activities and can inhibit the expression of inflammatory mediators such as tumor necrosis factor α (TNF-α). Punicic acid can also reduce the formation of β-amyloid deposits and hyperphosphorylation of tau by increasing the expression of GLUT4 protein and inhibiting the overactivation of calpain, and is used to prevent and treat neurodegenerative diseases. In addition, punicic acid also has breast cancer inhibitor properties that depend on lipid peroxidation and PKC pathways.
    Punicic acid
  • HY-N7056
    4'-Hydroxychalcone
    		Inhibitor 99.66%
    4'-Hydroxychalcone is a chalcone isolated from licorice root, with hepatoprotective activity. 4'-Hydroxychalcone inhibits TNFα-induced NF-κB activation via proteasome inhibition. 4'-Hydroxychalcone induces a rapid potassium release from mitochondrial vesicles and causes deterioration of respiratory control and oxidative phosphorylation of isolated rat liver mitochondria.
    4'-Hydroxychalcone
  • HY-N4225
    Aaptamine
    		Inhibitor 99.71%
    Aaptamine is an alkaloid that can be isolated from the sponge Aaptos suberitoides. Aaptamine is a competitive antagonist of the α-adrenergic receptor, as well as an inhibitor of the proteasome and cholinesterase. Aaptamine is cytotoxic to tumor cells and can induce apoptosis, cell cycle arrest of tumor cells, and the expression of p21 through a p53-independent pathway. Aaptamine has multiple activities such as anti-tumor, antioxidant, antibacterial, and analgesic effects.
    Aaptamine
  • HY-12370
    TY-51469
    		Inhibitor 99.79%
    TY-51469 is a chymase inhibitor with IC50s for simian and human chymases of 0.4 and 7.0 nM, respectively.
    TY-51469
  • HY-158412
    BT317
    		Inhibitor 99.81%
    BT317 is a blood-brain transmissible mitochondrial Lon peptidase I (LonP1) and CT-L proteasome inhibitor. BT317 can increase the production of reactive oxygen species (ROS) and induce apoptosis in astrocytoma cells. BT317 has antitumor activity.
    BT317
  • HY-109001
    Alicapistat
    		Inhibitor
    Alicapistat (ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD). Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC50 value of 395 nM.
    Alicapistat
  • HY-148732
    LU-005i
    		Inhibitor 98.24%
    LU-005i is a potent inhibitor of β5i subunit of immunoproteasomes (IC50 = 6.6 nM), selective over β5c subunit (IC50 = 287 nM).
    LU-005i
  • 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-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-B0914A
    10-Undecenoic acid zinc salt
    		Inhibitor 98.0%
    10-Undecenoic acid zinc salt (Undecylenic acid zinc salt) is an antifungal agent. 10-Undecenoic acid zinc salt inhibits Aβ oligomerization, scavenges ROS and inhibits μ-calpain activity. 10-Undecenoic acid zinc salt has neuroprotective effects. 10-Undecenoic acid zinc salt has anticancer effects on a variety of tumors. 10-Undecenoic acid zinc salt inhibits C. albicans biofilm formation and MRSA infection. 10-Undecenoic acid zinc salt inhibits quorum sensing signals of Bacillus subtilis and Pseudomonas aeruginosa.
    10-Undecenoic acid zinc salt
  • HY-108549
    clasto-Lactacystin β-lactone
    		Inhibitor 99.9%
    Clasto-Lactacystin β-lactone, a natural active metabolite of lactacystin, which is a metabolite of Streptomyces, acts as an irreversible 20S proteasome inhibitor.
    clasto-Lactacystin β-lactone
  • HY-135070
    Ac-RLR-AMC
    		98.91%
    Ac-RLR-AMC (Ac-Arg-Leu-Arg-AMC) 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
  • HY-P1081
    Acetyl-Calpastatin(184-210)(human)
    		Inhibitor 98.57%
    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-114170
    ML604440
    		Inhibitor 98.28%
    ML604440 is a specific and cell-permeable Proteasome β1i (LMP2) subunit inhibitor. ML604440 can be used in experimental colitis, EAE and autoimmune disease research. ML604440 shows synergistic effects and advantageous when combined with LMP7 inhibitor.
    ML604440
  • HY-W001023
    5-Amino-8-hydroxyquinoline
    5-Amino-8-hydroxyquinoline (5A8HQ; 5AHQ) is an orally active non-competitive 20S proteasome inhibitor. 5-Amino-8-hydroxyquinoline can inhibit NF-κB activity and induce cancer cells death and shows low cytotoxicity towards normal hematopoietic cells. 5-Amino-8-hydroxyquinoline can be used for the research of cancer, such as leukemia.
    5-Amino-8-hydroxyquinoline
Cat. No. Product Name / Synonyms Application Reactivity