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-P10003
    iso-VQA-ACC
    iso-VQA-ACC is a substrate for constitutive proteasome.
    iso-VQA-ACC
  • HY-P4291
    Z-Leu-Leu-Tyr-COCHO
    		Inhibitor
    Z-Leu-Leu-Tyr-COCHO is a potent chymotrypsin-like activity inhibitor with a Ki value of 3.0 nM.
    Z-Leu-Leu-Tyr-COCHO
  • HY-126743
    JBIR-22
    		Inhibitor
    JBIR-22 is a protein-protein interaction inhibitor of proteasome assembly factor 3 homodimer, which has the activity of inhibiting this interaction and exerting long-term cytotoxicity against human cervical cancer cell lines, and its stereochemical structure has been determined by total synthesis.
    JBIR-22
  • HY-P4348
    MeOSuc-Gly-Leu-Phe-AMC
    MeOSuc-Gly-Leu-Phe-AMC is a peptide substrate of proteasomal.
    MeOSuc-Gly-Leu-Phe-AMC
  • HY-117513
    CEP1612
    		Inhibitor
    CEP1612 is a dipeptidyl proteasome inhibitor with the IC50 of 60 nM. CEP1612 induces p21(WAF1)and p27(KIP1) expression and cell apoptosis. CEP1612 shows anticancer activity in vivo.
    CEP1612
  • HY-181498
    RAFKBP12
    		Ligand
    RAFKBP12 is a FKBP12 CAP-TAC (proteinase complex cap-targeted chimera) degrader. RAFKBP12 demonstrates the feasibility of the CAP-TAC strategy, which enables proteasome-dependent degradation of FKBP12 that is independent of E3 ubiquitin ligases and protein ubiquitination.
    RAFKBP12
  • HY-P1259
    PR-39
    		Inhibitor
    PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice.
    PR-39
  • HY-N2117R
    Isoginkgetin (Standard)
    		Inhibitor
    Isoginkgetin (Standard) is the analytical standard of Isoginkgetin. This product is intended for research and analytical applications. Isoginkgetin is a pre-mRNA splicing inhibitor inhibitor. Isoginkgetin also inhibits activities of both Akt, NF-κB and MMP-9. Isoginkgetin inhibits the activity of the 20S proteasome, induces apoptosis and activates autophagy.
    Isoginkgetin (Standard)
  • HY-151376
    SAP2-IN-1
    		Inhibitor
    SAP2-IN-1 is a secreted aspartic protease 2 (SAP2) inhibitor and has potent SAP2 inhibitory activity with an IC50 value of 0.92 μM. SAP2-IN-1 also is a virulence factor inhibitor and is inactive in vitro. SAP2-IN-1 can be used for the research of infection.
    SAP2-IN-1
  • HY-P11331
    Az-NC-002
    Az-NC-002 is a Proteasome trypsin-like site (β2) and immunoproteasome β2i-specific active probe. Az-NC-002 has weak off-target effects with no significant inhibition for Cathepsin D (HY-P2750), but this inhibition reacts outside of the active site or influence on a small fraction of the enzyme.
    Az-NC-002
  • HY-180131
    INVA8001
    		Inhibitor
    INVA8001 (ASB17061) is a highly selective and orally active chymase inhibitor with IC50 values for human chymase and mouse mast cell proteinase 4 (mMCP-4) of 0.02 and 0.03 μM, respectively. INVA8001 exhibits IC50 values for bovine α-chymotrypsin and human cathesin G of 3.4 and 32.1 μM, respectively, and it shows over 1000-fold selectivity for other related serine proteases. INVA8001 inhibits mast cells in a mouse primary sclerosing cholangitis (PSC) model, improves bile duct pathology, and alleviates bile stasis, demonstrating anti-inflammatory and anti-fibrotic effects.
    INVA8001
  • HY-N7890
    Isomoreollic acid
    		Control
    Isomoreollic acid is a cage xanthonoid. Isomoreollic acid exhibits cytotoxicity against colon cancer cells, with an IC50 > 10 μM for proteasome inhibition. Isomoreollic acid is present in the stem bark of Garcinia lateriflora. Isomoreollic acid can be used in colon cancer research.
    Isomoreollic acid
  • HY-182325
    DB-310
    		Inhibitor
    DB-310 is a selective immunoproteasome LMP2 inhibitor with an IC50 value of 80.62 nM. DB-310 inhibits the production of IL-1α in microglia. DB-310 improves cognitive function in the Tg2576 transgenic mouse model of Alzheimer's disease. DB-310 can be used for research related to Alzheimer's disease.
    DB-310
  • HY-123255
    BSc2118
    		Inhibitor
    BSc2118 is a 20S proteasome inhibitor with an IC50 of approximately 50 nM. BSc2118 induces G2/M phase cell cycle arrest and apoptosis in myeloma cells, inhibits cytoprotective autophagy, and suppresses tumor angiogenesis. BSc2118 reduces MMP9 activity, promotes angioneurogenesis, and alleviates recombinant tissue-type plasminogen activator-induced cerebral toxicity. BSc2118 is applicable to studies related to cerebral ischemia and multiple myeloma.
    BSc2118
  • HY-162754
    LMP7/LMP2-IN-1
    		Inhibitor
    LMP7/LMP2-IN-1 (Compound 19) is the orally active inhibitor for immunoproteasome subunits LMP7 and LMP2 with IC50 of 257 and 10 nM. LMP7/LMP2-IN-1 reduces the generation of antibody, downregulates the cells in spleen germinal center B and in plasma in NP-OVA-immunized mice, and can be used in research about autoimmune diseases.
    LMP7/LMP2-IN-1
  • HY-179394
    Immunoproteasome-IN-2
    		Inhibitor
    Immunoproteasome-IN-2 is selective immunoproteasome inhibitor with IC50 = 232.3 nM for LMP7, IC50 = 9384.9 nM for β5. Immunoproteasome-IN-2 exhibits ancillary inhibitory activity against LMP2 and MECL-1 subunits. Immunoproteasome-IN-2 demonstrates anti-inflammatory efficacy in a mouse model of arthritis and shows a favorable safety profile in toxicological studies with reduced hepatotoxicity and hematotoxicity. Immunoproteasome-IN-2 has LMP7/β5 selectivity directly correlated with lower systemic toxicity. Immunoproteasome-IN-2 can be employed for research in arthritis.
    Immunoproteasome-IN-2
  • HY-N14928
    Phepropeptin B
    		Inhibitor
    Phepropeptin B, a microbial secondary metabolite, is a proteasome inhibitor with an IC50 of 11 μg/mL.
    Phepropeptin B
  • HY-W409181
    (Rac)-PD 151746
    		Inhibitor
    (Rac)-PD 151746 is the optically inactive racemate of PD 151746 (HY-19749). PD 151746 is a neuroprotective calpain inhibitor with Ki values of 0.26 μM (u-calpain) and 5.33 μM (m-calpain), respectively.
    (Rac)-PD 151746
  • HY-156297
    β5i-IN-1
    		Inhibitor
    β5i-IN-1 is a potent and selective inhibitor of β5i with a IC50 of 8.463 nM. β5i-IN-1 releases TNF-α and IL-6 and influences the transcriptional activity of NF-κB. β5i-IN-1 can be used in study idiopathic pulmonary fibrosis.
    β5i-IN-1
  • HY-N2306R
    Aclacinomycin A (Standard)
    		Inhibitor
    Aclacinomycin A (Standard) is the analytical standard of Aclacinomycin A. This product is intended for research and analytical applications. Aclacinomycin A (Aclarubicin) is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A is an inhibitor of topoisomerase I and II. Aclacinomycin A inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis.
    Aclacinomycin A (Standard)
Cat. No. Product Name / Synonyms Application Reactivity