Proteasomes are very large protein complexes inside all eukaryotes and archaea, and in some bacteria.They are found in the cytoplasm and nucleus of eukaryotes. The proteasome's primary job is to break down unwanted or damaged proteins through the process of proteolysis, which is a peptide bond-breaking chemical reaction. Proteases are enzymes that carry out these types of reactions. A key mechanism by which cells control the concentration of specific proteins and destroy improperly folded proteins includes proteasomes. When a protein is degraded, it produces peptides that are seven to eight amino acids long. These peptides can then be further broken down into amino acids and used to create new proteins.A tiny protein called ubiquitin marks proteins for degradation. The tagging process is sped up by ubiquitin ligases, an enzyme family. Once a protein has one ubiquitin molecule attached to it, other ligases know to attach more ubiquitin molecules. As a result, a polyubiquitin chain forms, which the proteasome binds to and uses to break down the tagged protein.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V0684 | Bortezomib (PS-341; Velcade) | 179324-69-7 | Bortezomib (formerly also known as PS-341; trade name Velcade among others), a dipeptideboronic acid derivative, is cell-permeable, reversible, potent and highly selective inhibitor of 20S proteasome with potential antitumor activity. |
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V0686 | CARFILZOMIB (PR171) | 868540-17-4 | Carfilzomib (formerly also known as PR-171; trade name: Kyprolis) is a novel, potent, andirreversible proteasome inhibitor with potential antineoplastic activity. |
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V0693 | CELASTROL | 34157-83-0 | Celastrol (also called tripterine) is a naturally occurring pentacyclic nortriterpen quinone and a remedial ingredient found in the root extracts of Tripterygium Wilfordi (Thunder of God vine) and Celastrus Regelii. |
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V0692 | DELANZOMIB (CEP18770) | 847499-27-8 | Delanzomib (formerly known asCEP-18770) is a novel, potent, and orally bioactive inhibitor of the chymotrypsin-like (CL) activity of proteasome with potential antineoplastic activity. |
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V0689 | EPOXOMICIN (BU 4061T) | 134381-21-8 | Epoxomicin (formerly also known as BU-4061T) is a novel, potent, selective,cell-permeable and irreversible proteasome inhibitor with anti-inflammatory activity, it inhibits primarily the CH-L activity of the 20S proteasome, while T-L and PGPH catalytic activities are also inhibited at 100- and 1000-fold reduced rate. |
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V0688 | IXAZOMIB (MLN2238) | 1072833-77-2 | Ixazomib (formerly also known as MLN-2238) is a novel, potent, selective and reversible proteasome inhibitor (PI) with potential antineoplastic activity. |
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V33460 | Ixazomib citrate | 1239908-20-3 | Ixazomib citrate (MLN9708; MLN-9708; MLN 9708), the citrate salt and orally bioavailable prodrug of Ixazomib (MMLN2238; MMLN-2238), is a selective inhibitor of 20S proteasome (IC50 = 3.4 nM) with potential anticancer activity. |
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V0687 | Ixazomib citrate (MLN 9708; Ninlaro) | 1201902-80-8 | MLN9708 (also known as ixazomib citrate; MLN-9708; trade name Ninlaro),the citrate salt of Ixazomib(MMLN2238; MMLN-2238), isa prodrug of Ixazomib (MMLN-2238) which isan orally bioavailable and 2nd generation proteasome inhibitor (PI) with potential antineoplastic activity. |
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V2138 | Marizomib (Salinosporamide A; NPI-0052) | 437742-34-2 | Marizomib (formerly also known as ML-858, NPI-0052 and Salinosporamide A), anaturally-occurring salinosporamide extracted from the marine actinomycete Salinospora tropica, is a potent and selective 20S proteasome inhibitor (IC50 = 1.3 nM) with potential antineoplastic activity. |
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V0685 | MG-132 | 133407-82-6 | MG-132,a peptide aldehyde, is a novel, specific, potent, reversible, and cell-permeable inhibitor of proteasome with IC50 of 100 nM in a cell-free assay, and also inhibits calpain with IC50 of 1.2 μM. |
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V0559 | MG-132(R) | 1211877-36-9 | MG-132 (R) (R-isomer of MG-132),a peptide aldehyde, is a novel, potent, non-specific, cell permeable and reversible inhibitor 20S proteasome inhibitor, with IC50of 24.2 nM for the β5 chymotrypsin-like active site. |
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V0690 | ONX-0914 (PR-957) | 960374-59-8 | ONX-0914 (also known as ONX0914; PR957) is a selective inhibitor of LMP7 and LMP2 subunits of immunoproteasomes with the potential to be used inautoimmune diseases including rheumatoid arthritis, inflammatory bowel disease and lupus. |
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V0691 | OPROZOMIB (ONX-0912) | 935888-69-0 | Oprozomib (formerly known as ONX 0912 and PR 047) is a novel, potent, and orally bioavailable small molecule inhibitor for chymotrypsin-like (CT)-L activity of 20S proteasome β5/LMP7 with potential antitumor activity. |
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V0694 | PI-1840 | 1401223-22-0 | PI-1840 (PI1840; PI 1840) is a reversible/non-covalent and selective inhibitor of chymotrypsin-like (CT-L) activity of proteasome with potential anticancer activity. |
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V0695 | VR23 | 1624602-30-7 | VR23 (VR-23; VR 23) is a highly potent and selective inhibitor of trypsin-like proteasome with potential antitumor activity. |
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