Proteasome

Proteasome

货号 产品名 CAS号 信息
FB00444 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.
FB12106 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.
FB09985 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.
FB12085 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.
FB16793 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.
FB11810 Proteasome-IN-1 374080-21-4 Proteasome-IN-1 is a proteasome inhibitor extracted from patent WO 2013142376 A1.
FB08682 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.
FB08338 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.
FB06970 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).
FB02901 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.
FB05934 MG-132 133407-82-6 MG-132 is an inhibitor of proteasome (IC50 = 100 nM) and calpain (IC50 = 1.2 nM).
FB08133 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.
FB00107 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.
FB00239 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.
FB10922 GNF-6702 1799329-72-8 GNF-6702 is a proteasome inhibition for treatment of leishmaniasis, Chagas disease and sleeping sickness.
FB12542 Gliotoxin 67-99-2 Gliotoxin is an inhibitor of 20S proteasome and acts as immunosuppressive agent.
FB16057 Fulacimstat 1488354-15-9 Fulacimstat is a chymase inhibitor with IC50 values of 4nM and 3 nM for human and hamster chymase enzyme, respectively.
FB08107 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.
FB00108 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.
FB11984 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.
FB02540 Celastrol 34157-83-0 Celastrol is an inhibitor of HSP90 with antioxidant and anti-inflammatory activities.
FB01563 Carfilzomib 868540-17-4 Carfilzomib is an irreversible proteasome inhibitor with IC50 of < 5 nM and can treat relapsed and refractory multiple myeloma.
FB10774 Capzimin 2084868-04-0 Capzimin shows > 5-fold selectivity for Rpn11 over the related JAMM proteases and > 2 logs selectivity over several other metalloenzymes.
FB04399 Bortezomib 179324-69-7 Bortezomib is an inhibitor of 20S proteasome with Ki of 0.6 nM.
FB12254 AM 114 856849-35-9 AM 114 is an inhibitor of the chymotrypsin-like activity of the 20S proteasome with IC50 ~ 1 μM.
FB11135 Aclarubicin HCl 75443-99-1 Aclarubicin HCl is the HCl salt of aclarubicin, an oligosaccharide anthracycline antineoplastic antibiotic isolated from the bacterium Streptomyces galilaeus.
FB12586 (R)-MG 132 1211877-36-9 (R)-MG132 can act as an inhibitor of proteasome and be used in ubiquitination assay.
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