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-W273493
    4-Nitrochalcone
    4-Nitrochalcone (2-(4-Nitrobenzylidene)acetophenone) inhibits the proteasome, inhibits NF-κB activity induced by TNFα.
    4-Nitrochalcone
  • HY-N13904
    Argyrin A
    		Inhibitor
    Argyrin A, a cyclical peptide, is a potent antitumoral agent. Argyrin A exerts its effects through a potent inhibition of the proteasome. Argyrin A leads to increased endogenous p27kip1 levels by preventing protein turnover.
    Argyrin A
  • HY-N14927
    Phepropeptin A
    		Inhibitor
    Phepropeptin A, a microbial secondary metabolite, is a proteasome inhibitor with an IC50 of 21 μg/mL.
    Phepropeptin A
  • HY-N14929
    Phepropeptin C
    		Inhibitor
    Phepropeptin C, a microbial secondary metabolite, is a proteasome inhibitor with an IC50 of 12.5 μg/mL.
    Phepropeptin C
  • HY-168904
    BI-1942
    		Inhibitor
    BI-1942, a chemical probe, is a chymase inhibitor and has an IC50 of 0.4 nM for human chymase. BI-1942 can be used in the research of ophthalmic diseases.
    BI-1942
  • HY-101786R
    KZR-504 (Standard)
    		Inhibitor
    KZR-504 (Standard) is the analytical standard of KZR-504 (HY-101786). This product is intended for research and analytical applications. KZR-504 is a highly selective inhibitor of immunoproteasome low molecular mass polypeptide 2 (LMP2), with IC50s of 51 nM, 4.274 μM for LMP2 and LMP7, respectively. KZR-504 is of interest for the treatment of autoimmune disease.
    KZR-504 (Standard)
  • HY-179612
    SARS-CoV-2 3CLpro-IN-34
    		Inhibitor
    SARS-CoV-2 3CLpro-IN-34 (Compound 55) is a highly efficient non-covalent inhibitor of the SARS-CoV-2 3CLpro protease (b. SARS-CoV-2 3CLpro protease) with an IC50 of 1.9 μM. SARS-CoV-2 3CLpro-IN-34 can inhibit the 3CLpro protein of SARS-CoV-1, with its IC50 being 3.2 μM, and it shows high selectivity towards host cysteine proteases (such as cathepsins L/K and calpain). SARS-CoV-2 3CLpro-IN-34 exhibits antiviral activity in cells infected with SARS-CoV-2, with its EC50 being 25 μM, and it is not affected by P-gp inhibitors and shows no significant cytotoxicity. SARS-CoV-2 3CLpro-IN-34 can be used for research on SARS-CoV-2 infection.
    SARS-CoV-2 3CLpro-IN-34
  • HY-100739R
    RA190 (Standard)
    		Inhibitor
    RA190 (Standard) is the analytical standard of RA190 (HY-100739). This product is intended for research and analytical applications. RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.
    RA190 (Standard)
  • HY-100529R
    PD150606 (Standard)
    		Inhibitor
    PD150606 (Standard) is the analytical standard of PD150606 (HY-100529). This product is intended for research and analytical applications. PD 150606 is a selective, cell-permeable non-peptide calpain inhibitor with Ki values of 0.21 μM and 0.37 μM for μ- and m-calpains respectively, which is neuroprotective.
    PD150606 (Standard)
  • HY-B0914B
    10-Undecenoic acid (copper)
    		Inhibitor
    10-Undecenoic acid copper (Undecylenic acid copper) is an antifungal agent. 10-Undecenoic acid copper inhibits Aβ oligomerization, scavenges ROS and inhibits μ-calpain activity. 10-Undecenoic acid copper has neuroprotective effects. 10-Undecenoic acid copper has anticancer effects on a variety of tumors. 10-Undecenoic acid copper inhibits C. albicans biofilm formation and MRSA infection. 10-Undecenoic acid copper inhibits quorum sensing signals of Bacillus subtilis and Pseudomonas aeruginosa.
    10-Undecenoic acid (copper)
  • HY-113824
    RID-F
    		Inhibitor
    RID-F (Ridaifen-F), a Tamoxifen (HY-13757A) derivative, is a nonpeptidic proteasome inhibitor. RID-F inhibits human 20S proteasome activity, with IC50s of 0.64, 0.34, and 0.43 μM for CT-L, T-L, and PGPH, respectively.
    RID-F
  • HY-U00282
    Chymase-IN-2
    		Inhibitor
    Chymase-IN-2 is a chymase modulator which is useful in the treatment of inflammatory and serine protease mediated disorders.
    Chymase-IN-2
  • HY-U00362
    Neurodegenerative Disorder-Targeting Compound 1
    		Inhibitor
    Neurodegenerative Disorder-Targeting Compound 1 is a calpain inhibitor extracted from patent WO2010128102A1, compound example 63.
    Neurodegenerative Disorder-Targeting Compound 1
Cat. No. Product Name / Synonyms Application Reactivity