Proteasome

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Proteasome Inhibitors (12)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1013 Bortezomib (PS-341) Bortezomib (PS-341) is a potent 20S proteasome inhibitor with Ki of 0.6 nM in a cell-free assay.
  • Nat Med, 2014, 20(6):599-606
  • Cell Stem Cell, 2012, 11(2):242-52
  • Sci Transl Med, 2014, 6(250):250ra112
S2619 MG-132 MG-132 is an inhibitor of proteasome with IC50 of 100 nM in a cell-free assay, and also inhibits calpain with IC50 of 1.2 μM.
  • Nature, 2015, 528(7582):422-6
  • Immunity, 2016, 45(4):944
  • Nat Cell Biol, 2015, 17(1):95-103
S2853 Carfilzomib (PR-171) Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM in ANBL-6 cells, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities.
  • Nat Med, 2015, 10.1038/nm.3855
  • Sci Transl Med, 2014, 6(250):250ra112
  • J Clin Invest, 2014, 124(12):5263-74
S2181 MLN9708 MLN9708 immediately hydrolyzed to MLN2238, the biologically active form, on exposure to aqueous solutions or plasma. MLN2238 inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50/Ki of 3.4 nM/0.93 nM in cell-free assays, less potent to β1 and little activity to β2. Phase 3.
  • Mol Cell Proteomics, 2012, 11(12):1898-912
  • Cancer Lett, 2014, 343(2):286-94
  • Hemoglobin, 2014, 38(3):188-95
S2180 Ixazomib (MLN2238) MLN2238 inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50 and Ki of 3.4 nM and 0.93 nM in cell-free assays, respectively, also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites, with IC50 of 31 and 3500 nM. Phase 3.
  • Sci Transl Med, 2014, 6(250):250ra112
  • Cancer Lett, 2014, 343(2):286-94
  • J Cell Sci, 2012, 125(Pt 23):5733-44
S7038 Epoxomicin Epoxomicin is a selective proteasome inhibitor with anti-inflammatory activity, 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.
S7172 ONX-0914 (PR-957) ONX-0914 (PR-957) is a potent and selective immunoproteasome inhibitor with minimal cross-reactivity for the constitutive proteasome in a cell-free assay.
  • Parasite Immunol, 2015, 37(11):599-604
S7049 Oprozomib (ONX 0912) Oprozomib (ONX 0912) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM. Phase 1/2.
S7933 VR23 VR23 is a potent proteasome inhibitor with IC50 of 1 nM, 50-100 nM, and 3 μM for trypsin-like proteasomes, chymotrypsin-like proteasomes, and caspase-like proteasomes, respectively.
S7462 PI-1840 PI-1840 is a reversible and selective chymotrypsin-like (CT-L) inhibitor with IC50 of 27 nM with little effects on the other two major proteasome proteolytic activities, trypsin-like (T-L) and postglutamyl-peptide-hydrolysis-like (PGPH-L).
S1157 CEP-18770 (Delanzomib) CEP-18770 (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. Phase 1/2.
S1290 Celastrol Celastrol is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM.
  • Oncotarget, 2016, 7(20):29648-63

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1013 Bortezomib (PS-341) <1 mg/mL 76 mg/mL <1 mg/mL
S2619 MG-132 <1 mg/mL 95 mg/mL 95 mg/mL
S2853 Carfilzomib (PR-171) <1 mg/mL 50 mg/mL <1 mg/mL
S2181 MLN9708 <1 mg/mL 100 mg/mL <1 mg/mL
S2180 Ixazomib (MLN2238) <1 mg/mL 72 mg/mL 9 mg/mL
S7038 Epoxomicin <1 mg/mL 100 mg/mL 100 mg/mL
S7172 ONX-0914 (PR-957) <1 mg/mL 100 mg/mL 100 mg/mL
S7049 Oprozomib (ONX 0912) <1 mg/mL 100 mg/mL <1 mg/mL
S7933 VR23 <1 mg/mL 31 mg/mL <1 mg/mL
S7462 PI-1840 <1 mg/mL 78 mg/mL 33 mg/mL
S1157 CEP-18770 (Delanzomib) <1 mg/mL 83 mg/mL 83 mg/mL
S1290 Celastrol <1 mg/mL 90 mg/mL <1 mg/mL
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