Proteasome
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The proteasome is a large multisubunit complex of approximately 2.5 MDa that mediates a wide range of physiological and pathological cellular processes by selectively degrading unnecessary proteins in eukaryotes. The structure of a proteasome is comprised of the catalytic core particle (CP) and two terminal regulatory particles (RPs). The CP (also known as the 20S proteasome) is a barrel shaped multisubunit complex (approximately 750 kDa) consisting of four axially stacked heptameric rings (two outer α-rings and two inner β-rings) with 7 subunits in each ring, where three β subunits (β1, β2 and β5) contain catalytically active threonine residues and are associated with caspase-like, trypsin-like and chymotrypsin-like activities respectively.
Products Related to Proteasome(77)
- GA20483Ac-Arg-Leu-Arg-AMCCAS: 929903-87-7Purity: >98%
Ac-Arg-Leu-Arg-AMC is a fluorescent peptide substrate (excitation/emission wavelength=380/440-460nm) used to detect the trypsin-like activity of the 26S proteasome.
- GC10102Aclacinomycin ACAS: 57576-44-0Purity: ≥95%
An anthracycline with antibiotic and anticancer activities
- GC10342CalpeptinCAS: 117591-20-5Purity: >98.00%
Calpeptin is a reversible and cell-permeable cysteine cathepsin inhibitor. The ID 50 values of Calpeptin for calpain I and II (porcine), papain, and platelet calpain I are 52nM, 34nM, 138nM, and 20nM, respectively. Calpeptin alleviates apoptosis and secondary inflammatory changes in muscle cells.
- GC10486Salinosporamide A (NPI-0052, Marizomib)CAS: 437742-34-2Purity: >98.00%
Salinosporamide A (NPI-0052, Marizomib) is a 20S proteasome inhibitor isolated from the obligate marine actinobacterium Salinispora tropica , exhibiting potent antitumor activity with an IC 50 value of 1.3nM.
- GC11974Pepstatin ACAS: 26305-03-3Purity: >98.50%
Pepstatin A is an orally active inhibitor of aspartic proteases, which is produced by actinomycetes.
- GC12494EpoxomicinCAS: 134381-21-8Purity: >98.50%
Epoxomicin is a selective proteasome inhibitor that effectively inhibits the chymotrypsin-like (CH-L) activity of the 20S proteasome, with an IC 50 of approximately 40-80nM.
- GC12527MG-101 (Calpain Inhibitor I, ALLN)CAS: 110044-82-1Purity: >98.00%
MG-101 (Calpain Inhibitor I, ALLN) also known as Calpain Inhibitor I, selectively inhibits various cysteine proteases, including calpain I, calpain II, cathepsin B, and cathepsin L. The corresponding Ki values for these enzymes are 90pM, 220pM, 150pM, and 500pM.
- GC13123Lactacystin (Synthetic)CAS: 133343-34-7Purity: >95.00%
A selective inhibitor of the 20S proteasome
- GC15089Carfilzomib (PR-171)CAS: 868540-17-4Purity: >99.00%
Carfilzomib (PR-171) is a next-generation tetrapeptide epoxyketone proteasome inhibitor (IC 50 =5nM).
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC12003 | VR23 | 1624602-30-7 | >99.00% | |
proteasome inhibitor | ||||
| GC15802 | PI-1840 | 1401223-22-0 | >99.00% | |
Chymotrypsin-like (CT-L) inhibitor | ||||
| GA20483 | Ac-Arg-Leu-Arg-AMC | 929903-87-7 | >98% | |
Ac-Arg-Leu-Arg-AMC is a fluorescent peptide substrate (excitation/emission wavelength=380/440-460nm) used to detect the trypsin-like activity of the 26S proteasome. | ||||
| GC10102 | Aclacinomycin A | 57576-44-0 | ≥95% | |
An anthracycline with antibiotic and anticancer activities | ||||
| GC10178 | MG-115 | 133407-86-0 | >98.00% | |
MG-115 is a potent inhibitor with Kis of 21 nM and 35 nM for 20S and 26S proteasome, respectively. | ||||
| GC10342 | Calpeptin | 117591-20-5 | >98.00% | |
Calpeptin is a reversible and cell-permeable cysteine cathepsin inhibitor. The ID 50 values of Calpeptin for calpain I and II (porcine), papain, and platelet calpain I are 52nM, 34nM, 138nM, and 20nM, respectively. Calpeptin alleviates apoptosis and secondary inflammatory changes in muscle cells. | ||||
| GC10383 | MG-132 | 133407-82-6 | >98.00% | |
MG-132 is a potent proteasome and calpain inhibitor with IC 50 values of 100nM and 1.25μM, respectively. | ||||
| GC10486 | Salinosporamide A (NPI-0052, Marizomib) | 437742-34-2 | >98.00% | |
Salinosporamide A (NPI-0052, Marizomib) is a 20S proteasome inhibitor isolated from the obligate marine actinobacterium Salinispora tropica , exhibiting potent antitumor activity with an IC 50 value of 1.3nM. | ||||
| GC10561 | PD 151746 | 179461-52-0 | >98% | |
calpain inhibitor, cell-permeable | ||||
| GC11640 | MDL 28170 | 88191-84-8 | >97.00% | |
MDL 28170, a cell permeable, reversible, peptidic aldehyde inhibitor of calpain (K i = 0.01μM; K i for cathepsin B = 0.025μM). | ||||
| GC11974 | Pepstatin A | 26305-03-3 | >98.50% | |
Pepstatin A is an orally active inhibitor of aspartic proteases, which is produced by actinomycetes. | ||||
| GC12272 | CEP-18770 | 847499-27-8 | >98.00% | |
An inhibitor of chymotrypsin-like proteasome activity | ||||
| GC12494 | Epoxomicin | 134381-21-8 | >98.50% | |
Epoxomicin is a selective proteasome inhibitor that effectively inhibits the chymotrypsin-like (CH-L) activity of the 20S proteasome, with an IC 50 of approximately 40-80nM. | ||||
| GC12527 | MG-101 (Calpain Inhibitor I, ALLN) | 110044-82-1 | >98.00% | |
MG-101 (Calpain Inhibitor I, ALLN) also known as Calpain Inhibitor I, selectively inhibits various cysteine proteases, including calpain I, calpain II, cathepsin B, and cathepsin L. The corresponding Ki values for these enzymes are 90pM, 220pM, 150pM, and 500pM. | ||||
| GC12784 | Artemether (SM-224) | 71963-77-4 | >98.00% | |
An antiparasitic compound | ||||
| GC13123 | Lactacystin (Synthetic) | 133343-34-7 | >95.00% | |
A selective inhibitor of the 20S proteasome | ||||
| GC13711 | Gabexate mesylate | 56974-61-9 | >98.00% | |
A serine protease inhibitor | ||||
| GC13718 | MLN9708 | 1201902-80-8 | >98.00% | |
A prodrug form of MLN2238 | ||||
| GC13789 | AM 114 | 856849-35-9 | >98.50% | |
| GC13865 | PSI | 158442-41-2 | >98% | |
| GC15083 | Celastrol | 34157-83-0 | >99.50% | |
Celastrol is a proteasome inhibitor with a potent and preferred inhibition of purified 20S proteasome with an IC 50 of 2.5 μM. | ||||
| GC15089 | Carfilzomib (PR-171) | 868540-17-4 | >99.00% | |
Carfilzomib (PR-171) is a next-generation tetrapeptide epoxyketone proteasome inhibitor (IC 50 =5nM). | ||||
| GC15447 | Oprozomib (ONX-0912) | 935888-69-0 | >99.50% | |
An orally available proteasome inhibitor | ||||
| GC15517 | MG-262 | 179324-22-2 | >98% | |
A proteasome inhibitor with diverse biological activities | ||||
