2. Signalwege
  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.

Art. -Nr. Produktname Wirkung Reinheit Chemical Structure
  • HY-N11620
    Sadopeptins A
    		Inhibitor
    Sadopeptins A is a nature product that could be isolated from Streptomyces sp. Sadopeptins A is a potent proteasome inhibitor.
    Sadopeptins A
  • HY-P3414
    Proteasome-activating peptide 1
    		Activator
    Proteasome-activating peptide 1 is a peptide, which increases the chymotrypsin-like proteasomal catalytic activity and, consequently, proteolytic rates both in vitro and in culture. Proteasome-activating peptide 1 prevents protein aggregation in a cellular model of amyotrophic lateral sclerosis.
    Proteasome-activating peptide 1
  • HY-158197
    RC-106
    		Inhibitor
    RC-106 is a proteasome inhibitor (IC50: 35 μM) and Sigma receptor modulator with anticancer activity. RC-106 has antiproliferative activity against cancer cells including glioblastoma (GB) and multiple myeloma (MM).
    RC-106
  • HY-142920
    LMP7-IN-1
    		Inhibitor
    LMP7-IN-1, a Boronic acid derivative, is a potent and selective immunoproteasome subunit LMP7 (β5i) inhibitor with an IC50 of 1.83 nM (WO2021143923A1; compound 20).
    LMP7-IN-1
  • HY-P4293
    Z-Leu-Tyr-Chloromethylketone
    Z-Leu-Tyr-Chloromethylketone is a calpain inhibitor.
    Z-Leu-Tyr-Chloromethylketone
  • HY-181521
    RAPRMT5
    		Ligand
    RAPRMT5 is a PRMT5 CAP-TAC (proteinase complex-targeted chimeric agent) degrader. RAPRMT5 can induce PRMT5 to undergo proteasome-dependent, ubiquitin-independent degradation. RAPRMT5 can be used in the research of various cancers.
    RAPRMT5
  • HY-10227G
    Bortezomib (GMP)
    		Inhibitor
    Bortezomib (GMP) (PS-341 (GMP)) is Bortezomib (HY-10227) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Bortezomib can be used for the study of multiple myeloma (MM). Bortezomib effectively inhibits TREM2 expression in tumor-associated macrophages (TAMs).
    Bortezomib (GMP)
  • HY-129108
    9-cis-UAB30
    		Inhibitor
    9-cis-UAB30 is a rexinoid agonist. 9-cis-UAB30 significantly decreases the proliferation, viability, and motility of both patient-derived xenografts (PDXs). 9-cis-UAB30 induced cell-cycle arrest as demonstrated by the significant increase in the percentage of cells in G1 and a decrease in the percentage of cells in S phase by downregulating SKP2 and/or 20S proteasome activity, which leads to increased p27kip1 protein stability. 9-cis-UAB30 downregulates the abundance of stem cell marker mRNAs (Oct4, Nanog, Sox2, nestin) and upregulates the abundance of differentiation marker mRNAs (β3-tubulin, NSE, HOXC9, GAP43). 9-cis-UAB30 has no adverse effects on the central nervous system and cardiovascular system at the tested dose. 9-cis-UAB30 can be used for the study of neuroblastoma, cutaneous T-cell lymphomas, and breast cancer.
    9-cis-UAB30
  • HY-144369
    Proteasome-IN-4
    		Inhibitor
    Proteasome-IN-4 is an excellent and non-covalent proteasome inhibitor (IC50=8.39 nM). Proteasome-IN-4 has potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines. Proteasome-IN-4 can be used for cancer research.
    Proteasome-IN-4
  • HY-149514
    BC-05
    BC-05 is an orally active and potent inhibitor of CD13 and proteasome. BC-05 has an IC50 value of 0.13 μM for human CD13 and an IC50 value of 1.39 μM for the 20S proteasome. BC-05 can be used in multiple myeloma research.
    BC-05
  • HY-P1258A
    PSI TFA
    		Inhibitor
    PSI (TFA) is a potent proteasome inhibitor. PSI (TFA) inhibits the proliferation of primary effusion lymphoma (PEL) cells. PSI (TFA) can be used for the research of Kaposi’s sarcoma-associated herpesvirus (KSHV) infection and KSHV-associated lymphomas.
    PSI TFA
  • 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-181495
    RAJQ14
    RAJQ14 is a BRD4 PROTAC-like CAP-TAC (Proteasome Cap Targeting Chimeras) degrader. RAJQ14 binds to 19S proteasome cap subunits RPN1, RPN10, RPN13, and USP14 to recruit target proteins to the proteasome for ubiquitination-independent, proteasome-dependent degradation. RAJQ14 can be used for the research of cancer (Pink: BRD4 Ligand (HY-181496); Blue: Proteasome Ligand (HY-128978); Black: Linker).
    RAJQ14
  • 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-181523
    RA183
    		Ligand
    RA183 is a proteasome ligand that can be used to synthesize CAP-TAC (proteasome cap-targeted chimera), such as RAPRMT5 (HY-181521).
    RA183
  • 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-117520
    FV-162
    		Inhibitor
    FV-162 is a potent, orally active and irreversible proteasome inhibitor. FV-162 exhibits cytotoxic to human myeloma cell lines and primary myeloma cells. FV-162 inhibits tumor growth in a myeloma xenograft mouse model. FV-162 can be used for myeloma research.
    FV-162
Art. -Nr. Produktname / Synonyms Application Reactivity