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-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-P1259A
    PR-39 TFA
    		Inhibitor 99.96%
    PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice.
    PR-39 TFA
  • HY-119037
    UK-101
    		Inhibitor 99.58%
    UK-101 is a potent and selective immunoproteasome β1i (LMP2) inhibitor with an IC50 value of 104 nM, displays 144- and 10-fold selectivity over β1c (IC50=15 μM) and β5 subunit (IC50=1 μM), respectivey. UK-101 induces cell apoptosis and can be used for the study of prostate cancer.
    UK-101
  • HY-13207A
    ONX-0914 TFA
    		Inhibitor 98.01%
    ONX-0914 (PR-957) TFA is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 TFA blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 TFA is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (Ki=5.2 μM). ONX-0914 TFA reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1.
    ONX-0914 TFA
  • HY-119378
    AK 295
    		Inhibitor ≥99.0%
    AK 295 (CX 295) is a calpain inhibitor that inhibits apoptosis through a calpain-dependent pathway. AK 295 improves neurological function in a rat model of spinal cord injury (SCI). AK 295 can be used in the study of neurodegenerative diseases, such as bulbar amyotrophy, stroke, Alzheimer's disease, Parkinson's disease, multiple sclerosis.
    AK 295
  • HY-P10002
    EWFW-ACC
    EWFW-ACC is the tetrapeptide substrate for the immunoproteasome and has selectivity for the LMP7 subunits.
    EWFW-ACC
  • 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-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-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-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-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-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-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-135396
    (1S,2S)-Bortezomib
    		Inhibitor
    (1S,2S)-Bortezomib is an enantiomer of Bortezomib. Bortezomib is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki of 0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is an anti-cancer agent and the first therapeutic proteasome inhibitor to be used in humans.
    (1S,2S)-Bortezomib
  • HY-118933
    Calpain Inhibitor VI
    		Inhibitor 99.88%
    Calpain Inhibitor VI (SJA6017) is a synthesized peptide aldehyde inhibitor of calpain. Calpain Inhibitor VI inhibits purified m-calpain with the IC50 of 80 nM. Calpain Inhibitor VI can be used for the research of cataract.
    Calpain Inhibitor VI
  • HY-114419
    Zetomipzomib
    		Inhibitor
    Zetomipzomib (KZR-616), a first-in-class inhibitor of the immunoproteasome, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. Zetomipzomib has the potential for the research of multiple autoimmune diseases.
    Zetomipzomib
  • HY-148037
    Thrombin inhibitor 5
    		Inhibitor 99.82%
    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-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-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. Anti-cancer activity[1][2].
    Bortezomib-d<sub>8</sub>
  • HY-164027
    MyoMed 205
    		Inhibitor 98.00%
    MyoMed-205 is an inhibitor targeting the activity of MuRF1. MyoMed-205 prevents early diaphragmatic systolic dysfunction and atrophy due to unilateral diaphragmatic nerve denervation 12 hours later. MyoMed-205 reduces ubiquitination and subsequent proteasomal degradation of muscle proteins by inhibiting MuRF1 activity. MyoMed-205 increases levels of a protein that phosphorylates Akt (ser473), an important signaling molecule for muscle growth and maintenance. MyoMed-205 can be used to study and treat diaphragmatic dysfunction and atrophy (DIDD) caused by early apraxia, especially in clinical situations such as diaphragmatic paralysis or mechanical ventilation.
    MyoMed 205
Cat. No. Product Name / Synonyms Application Reactivity