2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Proteasome

Proteasome

Proteasome

Related Products

PDF 1.03 MB

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-13259
    MG-132
    		Inhibitor 99.97%
    MG-132 (Z-Leu-Leu-Leu-al) is a potent proteasome and calpain inhibitor with IC50s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, also is an autophagy activator. MG-132 also induces apoptosis.
    MG-132
  • HY-10227
    Bortezomib
    		Inhibitor 99.99%
    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.
    Bortezomib
  • HY-10455
    Carfilzomib
    		Inhibitor 99.98%
    Carfilzomib (PR-171) is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.
    Carfilzomib
  • HY-13067
    Celastrol
    		Inhibitor 99.90%
    Celastrol (Tripterine;Tripterin) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. In addition, Celastrol is also an antibiotic with potent antimicrobial activity against standard and clinical methicillin-resistant Staphylococcus aureus (MRSA) strains, inducing oxidative stress and inhibiting DNA synthesis by binding to P5CDH.
    Celastrol
  • HY-13259C
    (R)-MG-132
    		Inhibitor 99.97%
    (R)-MG-132 ((S,R,S)-(-)-MG-132) is the enantiomer of MG-132. (R)-MG-132 is a proteasome inhibitor with weaker cell cytotoxicity than MG-132.
    (R)-MG-132
  • HY-E70005H
    Collagenase, Type VIII
    Collagenase, Type VIII is a mixed enzyme derived from Clostridium histolyticum that contains collagenase, a nonspecific protease, and a clostripain. Collagenase, Type VIII can hydrolyze Type VIII collagen and may be used to study the formation of atherosclerosis. Type VIII collagen is a regulator of endothelial cell differentiation and angiogenesis, a substrate for cell adhesion and migration such as smooth muscle cells, and may accumulate in atherosclerosis. After endotoxin activates the expression of Collagenase, Type VIII, it can reduce the production of Type VIII collagen and has the potential to inhibit atherosclerosis.
    Collagenase, Type VIII
  • HY-P10003B
    iso-VQA-ACC acetate
    iso-VQA-ACC acetate is a substrate for constitutive proteasome.
    iso-VQA-ACC acetate
  • HY-162885
    YSY01A
    		Inhibitor
    YSY01A is a proteasome inhibitor that can suppress cancer cell survival by inducing apoptosis (Apoptosis). Its IC50 values are 51.0 nM for HEK293T, 9.2 nM for A549, 5.2 nM for MCF-7, 8.9 nM for MGC-803, and 35.4 nM for PC-3M cells. Additionally, YSY01A is also a degrader of gp130 and JAK2, and it eliminates constitutive STAT3 signaling by downregulating gp130 and JAK2 in human A549 lung cancer cells. YSY01A holds promise for research in the field of cancer therapy.
    YSY01A
  • HY-13821
    Epoxomicin
    		Inhibitor 99.69%
    Epoxomicin (BU-4061T) is an epoxyketone-containing natural product and a potent, selective and irreversible proteasome inhibitor. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. Epoxomicin has strongly antitumor and anti-inflammatory activity.
    Epoxomicin
  • HY-10453
    Ixazomib
    		Inhibitor 99.85%
    Ixazomib (MLN2238) is a selective, potent, and reversible proteasome inhibitor, which inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC50 of 3.4 nM (Ki of 0.93 nM).
    Ixazomib
  • HY-N2117
    Isoginkgetin
    		Inhibitor 99.95%
    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
  • HY-100223
    Calpeptin
    		Inhibitor ≥98.0%
    Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID50 of 40 nM for Calpain I in human platelets. Calpeptin is also an inhibitor of cathepsin K.
    Calpeptin
  • HY-13207
    ONX-0914
    		Inhibitor 99.72%
    ONX-0914 (PR-957) is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (Ki=5.2 μM). ONX-0914 reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1.
    ONX-0914
  • HY-10985
    Marizomib
    		Inhibitor 99.55%
    Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, pan-proteasome inhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC50=3.5, 28, and 430 nM, respectively).
    Marizomib
  • HY-18236
    MDL-28170
    		Inhibitor
    MDL-28170 (Calpain Inhibitor III) is a potent, selective and membrane-permeable cysteine protease inhibitor of calpain that rapidly penetrates the blood-brain barrier following systemic administration. MDL-28170 also block γ-secretase.
    MDL-28170
  • HY-18964
    MG-101
    		Inhibitor ≥98.0%
    MG-101 (ALLN) is an inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively. MG-101 induces apoptosis and inhibits tumor growth, it can be used for the research of colon cancer.
    MG-101
  • HY-10452
    Ixazomib citrate
    		Inhibitor 99.87%
    Ixazomib citrate (MLN9708) is a reversible inhibitor of the chymotrypsin-like proteolytic β5 site of the 20S proteasome with an IC50 of 3.4 nM and a Ki of 0.93 nM.
    Ixazomib citrate
  • HY-100529
    PD150606
    		Inhibitor 98.57%
    PD 150606 is a selective, cell-permeable non-peptide calpain inhibitor with Ki values of 0.21 μM and 0.37 μM for μ- and m-calpains respectively, which is neuroprotective.
    PD150606
  • HY-110404
    Capzimin
    		Inhibitor 99.21%
    Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor.
    Capzimin
  • HY-12113
    Oprozomib
    		Inhibitor 99.76%
    Oprozomib (PR-047) is an orally bioavailable and selective peptide epoxyketone proteasome inhibitor with IC50s of 36 and 82 nM for proteasome (β5) and immunoproteasome (LMP7), respectively. Oprozomib (ONX 0912) induces apoptosis in MM cells.
    Oprozomib
Cat. No. Product Name / Synonyms Application Reactivity