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-163770
    Anticancer agent 233
    		Inhibitor
    Anticancer agent 233 (compound 5g) is a 3,5-bis(arylmethylene)-4-piperidinone derivative with anticancer activity, with GI50 of 0.25 and 0.23 μM for cervical cancer (HeLa) and colon cancer (HCT116) cell lines, respectively. The chlorine atom on the aromatic ring of Anticancer agent 233 interacts well with the catalytic site of 20S proteasome, inhibiting the activity of 20S proteasome to exert its anticancer effect.
    Anticancer agent 233
  • HY-157033
    LMP7-IN-2
    		Inhibitor
    LMP7-IN-2 is a LMP7 inhibitor. LMP7-IN-2 can be used for associated inflammatory diseases and disorders.
    LMP7-IN-2
  • HY-180934
    AMC-3-030
    		Inhibitor
    AMC-3-030 is a selective and potent dual inhibitor targeting HDAC6 and chymotrypsin-like proteasome with IC50 values of 884 and 4.17 nM. AMC-3-030 has a proliferation inhibitory effect. AMC-3-030 can reduce α-tubulin and β-actin levels. AMC-3-030 can be used for research of multiple myeloma.
    AMC-3-030
  • HY-W001023A
    5-Amino-8-hydroxyquinoline dihydrochloride
    		Inhibitor
    5-Amino-8-hydroxyquinoline (5A8HQ; 5AHQ) dihydrochloride is an orally active non-competitive 20S proteasome inhibitor. 5-Amino-8-hydroxyquinoline dihydrochloride can inhibit NF-κB activity and induce cancer cells death and shows low cytotoxicity towards normal hematopoietic cells. 5-Amino-8-hydroxyquinoline dihydrochloride can be used for the research of cancer, such as leukemia.
    5-Amino-8-hydroxyquinoline dihydrochloride
  • HY-137286
    Z-Leu-Leu-Glu-βNA
    Z-Leu-Leu-Glu-βNA (Z-Leu-Leu-Glu-β-naphthylamide) is a substrate for determination of the glutamylpeptidyl-peptide hydrolase activity of the 20S proteasome.
    Z-Leu-Leu-Glu-βNA
  • HY-113221AS
    Isovalerylcarnitine-d3 chloride
    Isovalerylcarnitine-d3 chloride is the deuterium labeled Isovalerylcarnitine chloride (HY-145542). 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-d<sub>3</sub> chloride
  • HY-150591
    20S Proteasome-IN-3
    		Inhibitor
    20S Proteasome-IN-3 is a 20S proteasome β5 subunit inhibitor (IC50=1.64 μM). 20S Proteasome-IN-3 shows anti-tumor proliferation activity.
    20S Proteasome-IN-3
  • HY-158150
    20S Proteasome-IN-5
    		Inhibitor
    20S Proteasome-IN-5 (Compound 5) is a macrocyclic inhibitor of the 20S Proteasome, with IC50 values of 0.19 and 52.5 μM for ChT-L and PGPH-L activity, respectively.
    20S Proteasome-IN-5
  • HY-157035
    Proteasome β2c/i-IN-1
    		Inhibitor
    Proteasome β2c/i-IN-1 (compound 37) is a subunit-selective human proteasome β2c and β2i inhibitor .
    Proteasome β2c/i-IN-1
  • HY-19230
    DY-9760e
    		Inhibitor
    DY-9760e is a calmodulin (CaM) inhibitor. DY-9760e selectively inhibits the activity of various calmodulin-dependent enzymes by antagonizing the Ca²⁺/CaM complex, exhibiting the strongest inhibitory activity against nNOS, CaM kinase II, and calcineurin (Ki: 0.9, 1.4, and 2.0 μM, respectively). DY-9760e inhibits excessive nitric oxide production and protein tyrosine nitration, as well as the activation of calpain and caspase-3. DY-9760e reduces infarct size, improves cardiac function, and inhibits oxidative stress and cell death. DY-9760e can be used in research on the treatment of myocardial infarction, cerebral ischemia, and other diseases.
    DY-9760e
  • HY-168902
    Proteasome-IN-7
    		Inhibitor
    Proteasome-IN-7 (Compound 6f) is an epoxyketone macrocyclic peptidyl proteasome inhibitor (IC50 value of 37.92 nM for 20S proteasome ChT-L subunit). Proteasome-IN-7 displays robust antiproliferative effects against multiple myeloma, acute lymphoblastic leukemia and non-small cell lung cancer.
    Proteasome-IN-7
  • HY-138096
    Z-LLF-CHO
    		Inhibitor
    Z-LLF-CHO (Z-Leu-Leu-Phe-CHO) is a potent inhibitor of the chymotrypsin-like activity of the pituitary multicatalytic proteinase complex (Ki = 460 nM). Z-LLF-CHO is also a NF-κB nuclear translocation inhibitor.
    Z-LLF-CHO
  • HY-135511
    Nor-Cerpegin
    		Inhibitor
    Nor-Cerpegin is an analog of Cerpegin. Cerpegin, a pyridinone-fused c-lactone, is an inhibitor of 20S proteasome. Cerpegin can be used as a tranquillizer, anti-inflammatory, analgesic and antiulcer.
    Nor-Cerpegin
  • HY-170881
    TIR-199
    		Inhibitor
    TIR-199 is a novel and highly specific dual proteasome inhibitor that can effectively inhibit the PSMB5 subunit of constitutive proteasome and the PSMB8 subunit of immunoproteasome. TIR-199 can induce the death of various tumor cells. TIR-199 can be used for research on myeloma.
    TIR-199
  • HY-157212
    PARP-1/Proteasome-IN-1
    		Inhibitor
    PARP-1/Proteasome-IN-1 (compound 42i) is a dual PARP-1 and proteasome inhibitor with significant inhibitory effects on breast cancer. PARP-1/Proteasome-IN-1 can downregulate the expression of BRCA1 and RAD51 to inhibit homologous recombination repair function and induce apoptosis.
    PARP-1/Proteasome-IN-1
  • HY-N2166A
    Tomatine hydrochloride
    		Inhibitor
    Tomatine hydrochloride is a glycoalkaloid, found in the tomato plant (Lycopersicon esculentum Mill.). Tomatine hydrochloride elicits neurotoxicity in RIP1 kinase and caspase-independent manner. Tomatine hydrochloride promotes the upregulation of nuclear apoptosis inducing factor (AIF) in neuroblastoma cells. Tomatine hydrochloride also inhibits 20S proteasome activity.
    Tomatine hydrochloride
  • HY-183683
    DQ-9
    		Inhibitor
    DQ-9 is a selective immunoproteasome β5i inhibitor (IC50=0.0019 μM). DQ-9 generates additional inhibitory substances via iron-mediated intracellular activation, and induces oxidative stress, carbon-centered free radicals and macromolecular damage through its artemisinin domain. DQ-9 induces apoptosis in leukemia and multiple myeloma cells. DQ-9 exhibits selective cytotoxicity against leukemia and multiple myeloma cells by elevating the labile iron pool. DQ-9 can be used in the research of hematological malignancies (leukemia, multiple myeloma, mantle cell lymphoma, acute myeloid leukemia).
    DQ-9
  • HY-P2483
    Octaarginine
    		Inhibitor
    Octaarginine is a cell-penetrating peptide and proteasome inhibitor. Octaarginine exhibits mixed-type inhibition against 20S proteasome chymotrypsin-like, caspase-like, and trypsin-like activities, and inhibits 26S proteasome activity with decreased efficiency. Octaarginine induces ubiquitin-conjugated protein accumulation, mediates HSPG-dependent cellular internalization via macropinocytosis, enhances liposomal cargo uptake and gene delivery. Octaarginine can be used for the research of cervix carcinoma, collagen antibody-induced arthritis, and bacterial infections.
    Octaarginine
  • HY-156605
    Davelizomib
    		Inhibitor
    Davelizomib is proteasome inhibitor with antineoplastic effect.
    Davelizomib
  • HY-157032
    Proteasome-IN-5
    		Inhibitor
    Proteasome-IN-5 (compound 5) is a proteasome inhibitor.
    Proteasome-IN-5
Cat. No. Product Name / Synonyms Application Reactivity