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-P10030
    DPLG3
    		Inhibitor 99.18%
    DPLG3 is a specific chymotryptic-like β5i subunits inhibitor, with an IC50 of 4.5 nM. DPLG3 inhibits mouse i-20S with IC50 of 9.4 nM. DPLG3 downregulates the protein levels of NF-κB p50 and p65. DPLG3 can be used for immune disease research.
    DPLG3
  • HY-P1258
    PSI
    		Inhibitor
    PSI (Proteasome Inhibitor 1) is a potent proteasome inhibitor. PSI inhibits the proliferation of primary effusion lymphoma (PEL) cells. PSI has the potential for the research of Kaposi’s sarcoma-associated herpesvirus (KSHV) infection and KSHV-associated lymphomas.
    PSI
  • HY-120234
    Z-LLNle-CHO
    		Inhibitor
    Z-LLNle-CHO (Z-Leu-Leu-Nle-CHO) is a γ-secretase inhibitor I. Z-LLNle-CHO induces caspase and ROS-dependent apoptosis by blocking the Akt-mediated pro-survival pathway. Z-LLNle-CHO can be used in cancer research, such as breast cancer and leukaemia.
    Z-LLNle-CHO
  • HY-E70005L
    Collagenase (Type B, animal free)
    Collagenase (Type B, animal free) is a proteolytic enzyme targeting collagen, capable of releasing corneal endothelial cells (CECs) without damaging cell junctions.
    Collagenase (Type B, animal free)
  • HY-131350
    LXE408
    		Inhibitor 99.75%
    LXE408 is an orally active, non-competitive and kinetoplastid-selective proteasome inhibitor. LXE408 has an IC50 of 0.04 μM for L. donovani proteasome and an EC50 of 0.04 μM for L. donovani. LXE408 has a low propensity to cross the blood brain barrier. LXE408 has the potential for visceral leishmaniasis (VL) research.
    LXE408
  • HY-P10003B
    iso-VQA-ACC acetate
    		99.48%
    iso-VQA-ACC acetate is a substrate for constitutive proteasome.
    iso-VQA-ACC acetate
  • HY-P11306
    Biotin-(Oaa)3-epoxomicin
    		Inhibitor
    Biotin-(Oaa)3-epoxomicin is a biotin-labeled form of Epoxomicin (HY-13821), prepared by conjugating Epoxomicin with biotin via three hydrophilic oxaacetyl amino acid (Oaa) linkers. Biotin-(Oaa)3-epoxomicin is primarily used in proteomic studies for the capture, identification and target validation of proteasome complexes, to determine the intracellular targets of epoxomicin. Epoxomicin acts as a proteasome inhibitor and NF-κB inhibitor, which effectively blocks inflammatory responses in mouse ear edema assays. It inhibits proteasome activity via covalent binding to catalytic subunits including LMP7, X, MECL1 and Z, with the strongest inhibitory effect on chymotrypsin-like activity, and does not interfere with non-proteasomal proteases such as trypsin and papain.
    Biotin-(Oaa)3-epoxomicin
  • HY-P10714
    Ub4ix
    		Inhibitor 99.32%
    Ub4ix is a DUB/26S proteasome inhibitor. Ub4ix can protect K48-linked Ub chains from being chopped up by deubiquitinating enzymes (DUBs) and prevent the proteasomal degradation of Ub-tagged proteins. Ub4ix can reduce the viability of Hela cells and induce apoptosis, with an IC50 value of 1.6 μM.
    Ub4ix
  • HY-148037
    Thrombin inhibitor 5
    		Inhibitor 99.65%
    Thrombin inhibitor 5 (compound 385) is a thrombin inhibitor, with IC50s ranging from 0.1 μM to 1 μM. Thrombin inhibitor 5 can be used for research of venous thromboembolism.
    Thrombin inhibitor 5
  • HY-10227S
    Bortezomib-d8
    		Inhibitor 98.0%
    Bortezomib-d8 is the deuterium labeled Bortezomib. 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-d<sub>8</sub>
  • HY-119288
    BC-23
    		Inhibitor
    BC-23 (NSC 45382) is a proteasome inhibitor. BC-23 exhibits good inhibition of CT-L activity of the proteasome and is selective for malignant over normal cells.
    BC-23
  • HY-B0914R
    10-Undecenoic acid (Standard)
    		Inhibitor
    10-Undecenoic acid (Standard) is the analytical standard of 10-Undecenoic acid. This product is intended for research and analytical applications. 10-Undecenoic acid (Undecylenic acid) is an antifungal agent. 10-Undecenoic acid inhibits Aβ oligomerization, scavenges ROS and inhibits μ-calpain activity. 10-Undecenoic acid has neuroprotective effects. 10-Undecenoic acid has anticancer effects on a variety of tumors. 10-Undecenoic acid inhibits C. albicans biofilm formation and MRSA infection. 10-Undecenoic acid inhibits quorum sensing signals of Bacillus subtilis and Pseudomonas aeruginosa.
    10-Undecenoic acid (Standard)
  • HY-129867
    Z-Leu-Leu-Leu-AMC
    		98.4%
    Z-Leu-Leu-Leu-AMC is a fluorogenic substrate for measuring the chymotrypsin-like protease activity of the 20S proteasome.
    Z-Leu-Leu-Leu-AMC
  • HY-127102
    GSK3494245
    		Inhibitor 98.56%
    GSK3494245 (DDD01305143) is a potent, orally active, and selective inhibitor of the chymotrypsin-like activity of the parasite proteasome binding in a site sandwiched between the β4 and β5 subunits (IC50=0.16 μM for WT L. donovani proteasomes). GSK3494245 moderately inhibits chymotrypsin-like activity of human proteasome (IC50: purified 26S=13 µM; enriched THP-1 extracts IC50=40µM). GSK3494245 exhibits attractive biological and biosafety properties.
    GSK3494245
  • HY-10455S
    Carfilzomib-d8
    		Inhibitor 98.93%
    Carfilzomib-d8 is deuterium labeled Carfilzomib. Carfilzomib (PR-171) is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.
    Carfilzomib-d<sub>8</sub>
  • HY-144452
    Immunoproteasome inhibitor 1
    		Inhibitor 99.59%
    Immunoproteasome inhibitor 1 is a potent, reversible, time-independent immunoproteasome and proteasome inhibitor (Kis of 1.18, 0.27, 1.91 μM in β5c, β1i, β5i submits, respectively). Immunoproteasome inhibitor 1 can be used for the research of certain neoplastic diseases.
    Immunoproteasome inhibitor 1
  • HY-116171
    (Rac)-Calpain Inhibitor XII
    		Inhibitor 99.04%
    (Rac)-Calpain Inhibitor XII is a reversible and selective inhibitor of calpain I (μ-calpain, Ki=19 nM). (Rac)-Calpain Inhibitor XII has lower affinities for calpain II (m-calpain, Ki=120 nM) and cathepsin B (Ki=750 nM). (Rac)-Calpain Inhibitor XII has the potential for studying the role of calpains in diverse processes, including neutrophil chemotaxis, neuronal signaling, and cardiac response to injury.
    (Rac)-Calpain Inhibitor XII
  • HY-P3690
    Ac-Leu-Leu-Norleucinol
    		Inhibitor
    Ac-Leu-Leu-Norleucinol (ALLN) is a calpain inhibitor, can be used for research of Acetaminophen (HY-66005) induced acute liver damage, and lowers glutamic-oxalacetic transaminease (ALT) and glutamic-pyruvic transaminase (AST).
    Ac-Leu-Leu-Norleucinol
  • HY-W054146
    RAMB4
    		Inhibitor 98.02%
    RAMB4 is a ubiquitin-proteasome system (UPS)-stressor. RAMB4 inhibits ubiquitin-mediated protein degradation upstream of the 20S proteasomal catalytic activites. RAMB4 triggers a ubiquitin-proteasome-system (UPS)-stress response without affecting 20S proteasome catalytic activities. Anticancer activity.
    RAMB4
  • HY-109001A
    (1S,2R)-Alicapistat
    		Inhibitor 98.0%
    (1S,2R)-Alicapistat ((1S,2R)-ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD). (1S,2R)-Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC50 value of 395 nM.
    (1S,2R)-Alicapistat
Cat. No. Product Name / Synonyms Application Reactivity