2. Vías de señalización
  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. Nombre del producto Efecto Pureza Chemical Structure
  • HY-123051
    Ac-WLA-AMC
    		99.48%
    Ac-WLA-AMC is a specific 20S constitutive proteasome β5 fluorogenic substrate.
    Ac-WLA-AMC
  • HY-D1705
    Ac-ANW-AMC
    		98.88%
    Ac-ANW-AMC is a fluorogenic substrate for immunoproteasome. Ac-ANW-AMC can be used to measure β5i activity (Ex=345 nm, Em=445 nm).
    Ac-ANW-AMC
  • HY-123052
    Ac-PAL-AMC
    		99.90%
    Ac-PAL-AMC is a fluorogenic substrate specific for 20S proteasome LMP2/β1i activity.
    Ac-PAL-AMC
  • HY-W017227
    Alloxan hydrate
    		Inhibitor 99.99%
    Alloxan hydrate is a diabetogenic agent to induce diabetes. Alloxan hydrate is a proteasome inhibitor. Alloxan causes diabetes in experimental animals through its ability to destroy the insulin-secreting B-cells of the pancreas.
    Alloxan hydrate
  • HY-118355
    ALLM
    		Inhibitor 98.60%
    ALLM (Calpain inhibitor II) is a potent inhibitor of calpain and cathepsin proteases. ALLM inhibits neuronal cell death and improves chronic neurological function after spinal cord injury (SCI).
    ALLM
  • HY-111790
    M3258
    		Inhibitor 98.0%
    M3258 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 exerts high biochemical (IC50=3.6 nM) and cellular (IC50=3.4 nM) potency against the LMP7 subunit. M3258 shows strong antitumor efficacy in multiple myeloma xenograft models. M3258 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells.
    M3258
  • HY-19749
    PD 151746
    		Inhibitor
    PD151746 is a calpain inhibitor, shows a 20-fold selectivity for u-calpain (Ki = 0.
    PD 151746
  • HY-114419A
    Zetomipzomib maleate
    		Inhibitor 99.84%
    Zetomipzomib (KZR-616) maleate, a first-in-class immunoproteasome inhibitor, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP2/mLMP2) subunits of the immunoproteasome. Zetomipzomib maleate has the potential for the research of multiple autoimmune diseases.
    Zetomipzomib maleate
  • HY-12743A
    K-7174 dihydrochloride
    		Inhibitor 98.72%
    K-7174 dihydrochloride is an orally active proteasome and GATA inhibitor. K-7174 dihydrochloride is a cell adhesion inhibitor. K-7174 dihydrochloride induces cell apoptosis. K-7174 dihydrochloride shows antitumor activities, it can be used for the research of cancer.
    K-7174 dihydrochloride
  • HY-P3414A
    Proteasome-activating peptide 1 TFA
    		Activator 99.82%
    Proteasome-activating peptide 1 TFA is a peptide and a potent proteasome activator. Proteasome-activating peptide 1 TFA increases the chymotrypsin-like proteasomal catalytic activity and, consequently, proteolytic rates both in vitro and in culture. Proteasome-activating peptide 1 TFA prevents protein aggregation in a cellular model of amyotrophic lateral sclerosis.
    Proteasome-activating peptide 1 TFA
  • HY-10227R
    Bortezomib (Standard)
    		Inhibitor
    Bortezomib (Standard) is the analytical standard of Bortezomib. This product is intended for research and analytical applications. 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 (Standard)
  • HY-100739
    RA190
    		Inhibitor 99.04%
    RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.
    RA190
  • HY-B0914
    10-Undecenoic acid,98% (stabilized with TBC)
    		Inhibitor 99.99%
    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,98% (stabilized with TBC)
  • HY-18741
    VR23
    		Inhibitor 99.58%
    VR23 is a small molecule that potently inhibits the activities of trypsin-like proteasomes (IC50=1 nM), chymotrypsin-like proteasomes (IC50=50-100 nM), and caspase-like proteasomes (IC50=3 μM).
    VR23
  • HY-101786
    KZR-504
    		Inhibitor 99.33%
    KZR-504 is a highly selective inhibitor of immunoproteasome low molecular mass polypeptide 2 (LMP2), with IC50s of 51 nM, 4.274 μM for LMP2 and LMP7, respectively. KZR-504 is of interest for the treatment of autoimmune disease.
    KZR-504
  • HY-113221
    Isovalerylcarnitine
    		Activator 99.91%
    Isovalerylcarnitine is a metabolite of leucine. Isovalerylcarnitine can specifically activate calpain in human neutrophils. Isovalerylcarnitine inhibits tumor cell proliferation and induces apoptosis. Elevated circulating levels of Isovalerylcarnitine are negatively correlated with reduced lung cancer risk.
    Isovalerylcarnitine
  • HY-155482
    NA-184
    		Inhibitor 99.66%
    NA-184 is a selective and brain-penetrant calpain-2 inhibitor with an IC50 of 134 nM for mouse calpain-2. NA-184 has weak inhibitory activity on calpain-1 (IC50 of 2826 nM). NA-184 does not exhibit significant inhibition on a variety of other cysteine-, serine- or metallo-proteases. NA-184 shows significant neuroprotection and can be used for the study of traumatic brain injury (TBI).
    NA-184
  • HY-136750
    Z-LLY-FMK
    		Inhibitor 98.65%
    Z-LLY-FMK (Calpain Inhibitor IV) is a calpain inhibitor, involved in apoptosis of many cell systems. Z-LLY-FMK inhibits the intestine apoptosis after common bile duct ligation. Z-LLY-FMK reduces parasite burden in mice challenged with Taenia crassiceps cysts. Z-LLY-FMK can be used for the study of cysticercosis.
    Z-LLY-FMK
  • HY-157435
    PELI1-IN-1
    		Inhibitor 98.02%
    PELI1-IN-1 (compound 3d) is a potent inhibitor of PELI1, E3 ubiquitin ligase. PELI1-IN-1 has anti-tumPELI1-IN-1, a Resveratrol (HY-16561) derivative, is an orally active PELI1 Inhibitor (Kd = 8.2 μM). PELI1-IN-1 markedly interrupts the interaction of PELI1 and SNAIL/SLUG, and inhibits the K63-polyubiquitization of SNAIL/SLUG by PELI1, subsequently downregulating the protein levels of epithelial-mesenchymal transition (EMT) effectors SNAIL/SLUG. PELI1-IN-1 significantly reduces the level of SNAIL, SLUG and Vimentin without affecting the PELI1 expression. PELI1-IN-1 targets the FHA domain of PELI1 and disrupts the interaction, leading to the anti-metastasis of TNBC cells in vitro and in vivo. PELI1-IN-1 shows no evident toxicity in vivo.
    PELI1-IN-1
  • HY-108551
    MG-262
    		Inhibitor
    MG-262 (Z-Leu-Leu-LeuB(OH)2; ZL3B) is a reversible proteasome inhibitor. MG-262 down-regulates VEGF receptor Flt-1. MG-262 inhibits cell growth and induces apoptosis in malignant cells. MG-262 induces reactive oxygen species (ROS). MG-262 can be used for anti-cancer study.
    MG-262
Cat. No. Nombre del producto / Synonyms Application Reactivity