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.
Proteasome Related Products (37):
| Cat. No. |
Product Name |
Effect |
Purity |
-
- HY-13259
-
| MG-132
|
Inhibitor
|
>98.0%
|
|
MG-132 is a peptide aldehyde and a potent, reversible, and cell-permeable proteasome inhibitor with an IC50 of 100 nM, and effectively blocks the proteolytic activity of the 26S proteasome complex.
|
-
- HY-10227
-
| Bortezomib
|
Inhibitor
|
99.97%
|
|
Bortezomib (PS-341) is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib (PS-341) disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib (PS-341) is an anti-cancer drug and the first therapeutic proteasome inhibitor to be used in humans.
|
-
- HY-10455
-
| Carfilzomib
|
Inhibitor
|
99.96%
|
|
Carfilzomib is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.
|
-
- HY-13067
-
| Tripterin
|
Inhibitor
|
99.91%
|
|
Tripterin (Celastrol) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM.
|
-
- HY-13207
-
| ONX-0914
|
Inhibitor
|
98.86%
|
|
ONX-0914 (PR-957) is a potent and selective inhibitor of immunoproteasome subunit LMP7.
|
-
- HY-13259C
-
| (R)-MG-132
|
Inhibitor
|
>98.0%
|
|
(R)-MG-132 is the enantiomer of MG-132. (R)-MG-132 is a proteasome inhibitor with weaker cell cytotoxicity than MG-132. (S,R,S)-(-)-MG-132 stereoisomer is a more potent proteasome inhibitor than MG-132.
|
-
- HY-10985
-
| Marizomib
|
Inhibitor
|
|
|
Marizomib (Salinosporamide A) is 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).
|
-
- HY-114170
-
| ML604440
|
Inhibitor
|
|
|
ML604440 is a potent, specific and cell permeable proteasome β1i (LMP2) subunit inhibitor.
ML604440 impairs MHC class I cell surface expression, IL-6 secretion and differentiation of naïve T helper cells to T helper 17 cells. ML604440 strongly ameliorates disease in experimental colitis and EAE.
|
-
- HY-P0018A
-
| Pepstatin Trifluoroacetate
|
Inhibitor
|
99.11%
|
|
Pepstatin Trifluoroacetate is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin Ammonium also inhibits HIV protease.
|
-
- HY-10453
-
| Ixazomib
|
Inhibitor
|
99.24%
|
|
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).
|
-
- HY-13821
-
| Epoxomicin
|
Inhibitor
|
98.81%
|
|
Epoxomicin is a cell-permeable and irreversible proteasome inhibitor, primarily the chymotrypsin-like activity.
|
-
- HY-10452
-
| Ixazomib citrate
|
Inhibitor
|
>98.0%
|
|
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.
|
-
- HY-100529
-
| PD150606
|
Inhibitor
|
>98.0%
|
|
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.
|
-
- HY-18236
-
| MDL-28170
|
Inhibitor
|
>99.0%
|
|
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.
|
-
- HY-100739
-
| RA190
|
Inhibitor
|
99.47%
|
|
RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.
|
-
- HY-18964
-
| MG-101
|
Inhibitor
|
|
|
MG-101 is a potent 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.
|
-
- HY-12113
-
| Oprozomib
|
Inhibitor
|
99.60%
|
|
Oprozomib (ONX 0912; PR047) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM.
|
-
- HY-10454
-
| Delanzomib
|
Inhibitor
|
>98.0%
|
|
Delanzomib(CEP-18770) is a novel orally-active inhibitor of the chymotrypsin-like activity of the proteasome that down-modulates the nuclear factor-kappaB (NF-kappaB) activity.
|
-
- HY-110404
-
| Capzimin
|
Inhibitor
|
99.19%
|
|
Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor.
|
-
- 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.
|
