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Proteasome

Proteasome

货号 产品名 CAS号 信息
CSN17237 VR23 1624602-30-7 VR23 is a small molecule inhibitor which targets β2 of the 20S proteasome with IC50 of 1 nM and can induce apoptosis of cancer cells via cyclin E–mediated 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 (β1, β2, and β5) 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 ± 0.14 nM) over trypsin-like and peptidylglutamyl peptide hydrolyzing (IC50 values > 100 μM) 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 β5 (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 = 1.2 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 (β5) site of 20S proteasome with IC50 and Ki of 3.4 nM and 0.93 nM, respectively.
CSN17356 Ixazomib citrate 1239908-20-3 Ixazomib citrate is the citrate form of ixazomib which is an inhibitor of chymotrypsin-like proteolytic (β5) 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.
CSN22831 Gliotoxin 67-99-2 Gliotoxin is an inhibitor of 20S proteasome and acts as immunosuppressive agent.
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.
CSN15770 Epoxomicin 134381-21-8 Epoxomicin is a potent anti-tumor agent isolated from Actinomycetes that is used as a selective and irreversible inhibitor of the 20S proteasome.
CSN12951 Delanzomib 847499-27-8 Delanzomib is an orally active inhibitor of the chymotrypsin-like activity of proteasome with IC50 of 3.8 nM, with only marginal inhibition of the tryptic and peptidylglutamyl activities of the proteosome.
CSN22376 Clasto-Lactacystin β-lactone 154226-60-5 Clasto-Lactacystin β-lactone, a natural active metabolite of lactacystin, which is a metabolite of Streptomyces, acts as an irreversible 20S proteasome inhibitor.
CSN16303 Tripterin 34157-83-0 Celastrol is an inhibitor of HSP90 with antioxidant and anti-inflammatory activities.
CSN13893 Carfilzomib 868540-17-4 Carfilzomib is an irreversible proteasome inhibitor with IC50 of < 5 nM and can treat relapsed and refractory multiple myeloma.
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 mg/mL 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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