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Proteasome
| Cat. No. | Product Name | CAS No. | Information |
|---|---|---|---|
| CSN17237 | VR23 | 1624602-30-7 | VR23 is a small molecule inhibitor which targets 2 of the 20S proteasome with IC50 of 1 nM and can induce apoptosis of cancer cells via cyclin Emediated centrosome amplification |
| CSN22527 | TY-51469 | 603987-59-3 | TY-51469 is a chymase inhibitor with IC50s for simian and human chymases of 0.4 and 7.0 nM, respectively. |
| CSN18857 | TIR-199 | 1514925-83-7 | TIR-199 a natural product-derived syrbactin structural analog which covalently binds each of the three catalytic subunits 1 2 and 5 and revealed key interaction sites and is used for the treatment of multiple myeloma and other forms of cancer |
| CSN22501 | Rpn11-IN-1 | 2084867-65-0 | Rpn11-IN-1 is a potent and selective inhibitor of proteasome subunit Rpn11 with an IC50 of 390 nM |
| CSN26934 | RA190 | 1617495-03-0 | RA190 is a potent Rpn13 inhibitor and ADRM1 Inhibitor, Suppressing Intrahepatic Cholangiocarcinoma by Inducing NF-kappaB-Mediated Cell Apoptosis. RA190 represents a novel class of proteasome inhibitor that covalently binds to cysteine 88 of RPN13, an ubiquitin receptor subunit of the proteasome's 19S regulatory particle. RA190 treatment inhibits proteasome function, causing rapid accumulation of polyubiquitinated proteins. RA190 has therapeutic activity in a xenograft model, and with sorafenib exhibited synergetic killing of HCC cells in vitro, suggesting further exploration of such a combination treatment of HCC is warranted. |
| CSN25332 | RAMB4 | 145888-79-5 | PTP1B-IN-9 is a ubiquitin-proteasome system (UPS)-stressor. It inhibits ubiquitin-mediated protein degradation upstream of the 20S proteasomal catalytic activites, with anticancer activity. |
| CSN22188 | Proteasome-IN-1 | 374080-21-4 | Proteasome-IN-1 is a proteasome inhibitor extracted from patent WO 2013142376 A1 |
| CSN11777 | Procyanidin A2 | 41743-41-3 | Procyanidin A2, a natural product isolated and purified from the rhizomes of Belamcanda chinensis (L.) DC., blocks apoptosis pathways, by exerting its effects by promoting rpn-3 expression to enhance the activity of proteasomes and down-regulating egl-1 expression, and has anti-inflammatory mechanism in LPS-activated RAW 264.7 macrophages, by reducing the transcriptional and translational levels of inducible nitric oxide synthase (iNOS) as well as the production of NO. |
| CSN15914 | PI-1840 | 1401223-22-0 | PI-1840 is a potent and selective inhibitor for chymotrypsin-like CT-L IC50 value 27 014 nM over trypsin-like and peptidylglutamyl peptide hydrolyzing IC50 values 100 M activities of the proteasome |
| CSN15835 | ONX-0914 | 960374-59-8 | ONX-0914 is 20- to 40-fold more selective for LMP7 over the next most sensitive sites, β5 or LMP2. |
| CSN18603 | Oprozomib | 935888-69-0 | ONX 0912 is an inhibitor of proteasome that targets the chymotrypsin-like activity of the 20S proteasome subunits 5 (IC50 36 nM) and LMP7 (IC50 82 nM). |
| CSN17316 | Ixazomib Citrate (MLN9708) Analogue | 1201902-80-8 | MLN9708 is the prodrug of MLN2238 which is an inhibitor of the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50 and Ki of 3.4 nM, 0.93 nM, respectively. |
| CSN11436 | MG-132 | 133407-82-6 | MG-132 is an inhibitor of proteasome IC50 100 nM and calpain IC50 12 nM |
| CSN19716 | Marizomib | 437742-34-2 | Marizomib, a natural product isolated and purified from marine bacteria Salinispora tropica and Salinispora arenicola, inhibits 20S proteasome to overcome compensatory hyperactivation in multiple myeloma and solid tumour patients. |
| CSN26247 | N-Acetyl-S-((2R,3S,4R)-3-hydroxy-2-((S)-1-hydroxy-2-methylpropyl)-4-methyl-5-oxopyrrolidine-2-carbonyl)-L-cysteine | 133343-34-7 | Lactacystin is a potent and selective proteasome inhibitor with an IC50 of 4.8 μM for 20S proteasome found in Streptomyces. Lactacystin also inhibits the lysosomal enzyme cathepsin A. |
| CSN12950 | Ixazomib | 1072833-77-2 | Ixazomib selectively inhibits the chymotrypsin-like proteolytic 5 site of 20S proteasome with IC50 and Ki of 34 nM and 093 nM respectively |
| CSN17356 | Ixazomib citrate | 1239908-20-3 | Ixazomib citrate is the citrate form of ixazomib which is an inhibitor of chymotrypsin-like proteolytic (5) site of the 20S proteasome with IC50 of 3.4 nM. |
| CSN19673 | GNF6702 | 1799329-72-8 | GNF-6702 is a proteasome inhibition for treatment of leishmaniasis Chagas disease and sleeping sickness |
| CSN24826 | Fulacimstat | 1488354-15-9 | Fulacimstat is a chymase inhibitor with IC50 values of 4nM and 3 nM for human and hamster chymase enzyme, respectively. |
| CSN12951 | Delanzomib | 847499-27-8 | Delanzomib is an orally active inhibitor of the chymotrypsin-like activity of proteasome with IC50 of 38 nM with only marginal inhibition of the tryptic and peptidylglutamyl activities of the proteosome |
| CSN22376 | Clasto-Lactacystin β-lactone | 154226-60-5 | Clasto-Lactacystin -lactone, a natural active metabolite of lactacystin, which is a metabolite of Streptomyces, acts as an irreversible 20S proteasome inhibitor. |
| CSN19285 | Capzimin | 2084868-04-0 | Capzimin shows 5-fold selectivity for Rpn11 over the related JAMM proteases and 2 logs selectivity over several other metalloenzymes |
| CSN14664 | Broussonin B | 73731-86-9 | Broussonin B, a natural product isolated and purified from the branch of Broussonetia papyrifera, induces neurite outgrowth in PC-12 cells at concentration of 50 mgmL and shows moderate inhibitory activities against a chymotrypsin-like activity of the proteasome. |
| CSN10115 | Bortezomib | 179324-69-7 | Bortezomib is an inhibitor of 20S proteasome with Ki of 0.6 nM. |
| CSN22676 | Proteasome inhibitor IX | 856849-35-9 | AM 114 is an inhibitor of the chymotrypsin-like activity of the 20S proteasome with IC50 ~ 1 μM. |
| CSN20399 | Aclacinomycin A hydrochloride | 75443-99-1 | Aclarubicin HCl is the HCl salt of aclarubicin, an oligosaccharide anthracycline antineoplastic antibiotic isolated from the bacterium Streptomyces galilaeus. |
| CSN22627 | (R)-MG-132 | 1211877-36-9 | (R)-MG132 can act as an inhibitor of proteasome and be used in ubiquitination assay. |
| CSN50059 | MG-262 | 179324-22-2 | |
| CSN67087 | 20S Proteasome-IN-1 | 858557-69-4 |
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