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Proteasome

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
CSN25332 3,5-Bis(3,4-dichlorobenzylidene)piperidin-4-one 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
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 MLN9708 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.
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 GNF-6702 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 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.
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 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 AM 114 856849-35-9 AM 114 is an inhibitor of the chymotrypsin-like activity of the 20S proteasome with IC50 ~ 1 μM.
CSN20399 Aclarubicin HCl 75443-99-1 Aclarubicin HCl is the HCl salt of aclarubicin, an oligosaccharide anthracycline antineoplastic antibiotic isolated from the bacterium Streptomyces galilaeus.
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