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Catalog No. Product Name Information Product Use Citations Product Validations
S1013 Bortezomib (PS-341) Bortezomib (PS-341, Velcade, LDP-341, MLM341, NSC 681239) is a potent 20S proteasome inhibitor with Ki of 0.6 nM. It exhibits favorable selectivity towards tumor cells over normal cells. Bortezomib (PS-341) inhibits NF-κB and induces ERK phosphorylation to suppress cathepsin B and inhibit the catalytic process of autophagy in ovarian cancer and other solid tumors.
Sci Immunol, 2022, 7(68):eabi6763
Sci Adv, 2022, 8(4):eabi7711
Nat Commun, 2022, 13(1):1009
S1157 Delanzomib (CEP-18770) Delanzomib (CEP-18770) 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.
Pharmaceutics, 2021, 13(3)314
Autophagy, 2020, 10.1080/15548627.2020.1740529
Cell Death Dis, 2020, 11(9):783
S1290 Celastrol (NSC 70931) Celastrol (NSC 70931, Tripterine) is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. Celastrol induces apoptosis and autophagy via the ROS/JNK signaling pathway. Celastrol inhibits dopaminergic neuronal death of Parkinson's disease through activating mitophagy.
Mol Oncol, 2021, 10.1002/1878-0261.12936
Aging (Albany NY), 2021, 13(12):16816-16833
Molecules, 2021, 26(14)4124
S2180 Ixazomib (MLN2238) Ixazomib (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. Ixazomib (MLN2238) induces autophagy. Phase 3.
Cell Death Dis, 2022, 13(3):197
Clin Cancer Res, 2021, 27(5):1410-1420
Pharmaceutics, 2021, 13(3)314
S2181 Ixazomib Citrate (MLN9708) Analogue Ixazomib Citrate (MLN9708) Analogue is the analogue of Ixazomib Citrate (MLN9708) from WO2016165677A1. Ixazomib Citrate (MLN9708) immediately hydrolyzed to Ixazomib (MLN2238), the biologically active form, on exposure to aqueous solutions or plasma. Ixazomib (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. Ixazomib (MLN2238) induces autophagy. Phase 3.
Autophagy, 2021, 1-19
Cell Chem Biol, 2021, S2451-9456(21)00400-1
S2619 MG-132 MG132 (Z-Leu-Leu-Leu-al) is a potent cell-permeable proteasome and calpain inhibitor with IC50s of 0.1 μM and 1.2 μM for the inhibition of proteasome and calpain, respectively. MG132 activates autophagy and induces apoptosis in tumor cells.
Nature, 2022, 603(7902):721-727
Signal Transduct Target Ther, 2022, 7(1):35
Mol Cell, 2022, S1097-2765(22)00085-5
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. Carfilzomib activates prosurvival autophagy and induces cell apoptosis.
Mol Cell, 2022, 82(3):585-597.e11
Cell Death Differ, 2022, 10.1038/s41418-022-00942-z
Cell Death Dis, 2022, 13(3):197
S4432 Ixazomib Citrate (MLN9708) Ixazomib citrate (MLN9708, Ninlaro) is a prodrug of Ixazomib (MLN2238), which is a selective, orally bioavailable inhibitor of 20S proteasome that inhibits the chymotrypsin-like proteolytic (β5) site with IC50 of 3.4 nM and Ki of 0.93 nM, respectively. Ixazomib (MLN2238) also inhibits caspase-like (β1) and trypsin-like (β2) proteolytic sites with IC50 of 31 nM and 3500 nM, respectively.
Cell Death Dis, 2022, 13(3):197
Clin Cancer Res, 2021, 27(5):1410-1420
Oncogene, 2019, 38(16):3047-3060
S5813 Isoginkgetin Isoginkgetin is a naturally derived biflavonoid with anti-tumor activity. Isoginkgetin directly inhibits the chymotrypsin-like, trypsin-like, and caspase-like activities of the 20S proteasome. Isoginkgetin also is a general inhibitor of Pre-mRNA splicing.
S6851 RA-190 RA190, a bis-benzylidine piperidon, is a potent, selective and oral effective inhibitor of proteasome ubiquitin receptor RPN13/ADRM1 with anticancer activity. RA190 triggers ER stress response, p53/p21 signaling axis and autophagy in multiple myeloma cells.
S7038 Epoxomicin (BU-4061T) Epoxomicin (BU-4061T, Aids010837) 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. Epoxomicin promotes apoptosis.
Oxid Med Cell Longev, 2022, 2022:5044046
Neurosci Bull, 2022, 10.1007/s12264-022-00818-9
Cell Biol Toxicol, 2022, 10.1007/s10565-022-09699-0
S7049 Oprozomib (ONX 0912) Oprozomib (ONX 0912, PR-047) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM. Phase 1/2.
Mol Ther Nucleic Acids, 2022, 27:335-348
Pharmaceutics, 2021, 13(3)314
Autophagy, 2020, 10.1080/15548627.2020.1740529
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.
Oncol Rep, 2021, 45(4)34
Sci Rep, 2020, 10(1):15765
J Clin Pathol, 2020, jclinpath-2020-206618
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).
Nat Cell Biol, 2022, 24(3):364-372
Cancer Sci, 2020, 112(1):133-143
Oncol Rep, 2019, 41(5):2803-2817
S7504 Salinosporamide A (NPI-0052) Salinosporamide A (NPI-0052, ML858, Marizomib, MRZ) is a novel marine derived proteasome inhibitor which inhibits CT-L β5, C-L β1, and T-L β2 proteasome activities in human erythrocyte-derived 20S proteasomes with IC50 of 3.5 nM, 430 nM, 28 nM.
Mol Cancer Res, 2020, 18(7):1004-1017
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.
Autophagy, 2021, 1-19
Cancer Sci, 2020, 112(1):133-143
Sci Rep, 2018, 8(1):671
S8279 Shikonin (C.I. 75535) Shikonin (C.I. 75535, Anchusin, Anchusa acid, Alkanna Red, Isoarnebin 4, NSC 252844), a potent and specific Pyruvate kinase M2 (PKM2) inhibitor, is a major component of zicao (purple gromwell, the dried root of Lithospermum erythrorhizon), a Chinese herbal medicine with various biological activities. It is also an inhibitor of TMEM16A chloride channel activity using cell-based fluorescent-quenching assay. Shikonin exerts an anti-inflammatory effect by inhibiting tumor necrosis factor-α (TNF-α) and prevents activation of nuclear factor-κB (NF-κB) pathway via proteasome inhibition.
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Bioengineered, 2022, 13(3):5928-5941
S3269 Acetylcorynoline Acetylcorynoline, a major alkaloid component derived from Corydalis bungeana which is a traditional Chinese medical herb, shows anti-inflammatory properties. Acetylcorynoline may decrease egl-1 expression to suppress apoptosis pathways and increase rpn5 expression to enhance the activity of proteasomes.
S1013 Bortezomib (PS-341) Bortezomib (PS-341, Velcade, LDP-341, MLM341, NSC 681239) is a potent 20S proteasome inhibitor with Ki of 0.6 nM. It exhibits favorable selectivity towards tumor cells over normal cells. Bortezomib (PS-341) inhibits NF-κB and induces ERK phosphorylation to suppress cathepsin B and inhibit the catalytic process of autophagy in ovarian cancer and other solid tumors.
Sci Immunol, 2022, 7(68):eabi6763
Sci Adv, 2022, 8(4):eabi7711
Nat Commun, 2022, 13(1):1009
S1157 Delanzomib (CEP-18770) Delanzomib (CEP-18770) 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.
Pharmaceutics, 2021, 13(3)314
Autophagy, 2020, 10.1080/15548627.2020.1740529
Cell Death Dis, 2020, 11(9):783
S1290 Celastrol (NSC 70931) Celastrol (NSC 70931, Tripterine) is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. Celastrol induces apoptosis and autophagy via the ROS/JNK signaling pathway. Celastrol inhibits dopaminergic neuronal death of Parkinson's disease through activating mitophagy.
Mol Oncol, 2021, 10.1002/1878-0261.12936
Aging (Albany NY), 2021, 13(12):16816-16833
Molecules, 2021, 26(14)4124
S2180 Ixazomib (MLN2238) Ixazomib (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. Ixazomib (MLN2238) induces autophagy. Phase 3.
Cell Death Dis, 2022, 13(3):197
Clin Cancer Res, 2021, 27(5):1410-1420
Pharmaceutics, 2021, 13(3)314
S2181 Ixazomib Citrate (MLN9708) Analogue Ixazomib Citrate (MLN9708) Analogue is the analogue of Ixazomib Citrate (MLN9708) from WO2016165677A1. Ixazomib Citrate (MLN9708) immediately hydrolyzed to Ixazomib (MLN2238), the biologically active form, on exposure to aqueous solutions or plasma. Ixazomib (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. Ixazomib (MLN2238) induces autophagy. Phase 3.
Autophagy, 2021, 1-19
Cell Chem Biol, 2021, S2451-9456(21)00400-1
S2619 MG-132 MG132 (Z-Leu-Leu-Leu-al) is a potent cell-permeable proteasome and calpain inhibitor with IC50s of 0.1 μM and 1.2 μM for the inhibition of proteasome and calpain, respectively. MG132 activates autophagy and induces apoptosis in tumor cells.
Nature, 2022, 603(7902):721-727
Signal Transduct Target Ther, 2022, 7(1):35
Mol Cell, 2022, S1097-2765(22)00085-5
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. Carfilzomib activates prosurvival autophagy and induces cell apoptosis.
Mol Cell, 2022, 82(3):585-597.e11
Cell Death Differ, 2022, 10.1038/s41418-022-00942-z
Cell Death Dis, 2022, 13(3):197
S4432 Ixazomib Citrate (MLN9708) Ixazomib citrate (MLN9708, Ninlaro) is a prodrug of Ixazomib (MLN2238), which is a selective, orally bioavailable inhibitor of 20S proteasome that inhibits the chymotrypsin-like proteolytic (β5) site with IC50 of 3.4 nM and Ki of 0.93 nM, respectively. Ixazomib (MLN2238) also inhibits caspase-like (β1) and trypsin-like (β2) proteolytic sites with IC50 of 31 nM and 3500 nM, respectively.
Cell Death Dis, 2022, 13(3):197
Clin Cancer Res, 2021, 27(5):1410-1420
Oncogene, 2019, 38(16):3047-3060
S5813 Isoginkgetin Isoginkgetin is a naturally derived biflavonoid with anti-tumor activity. Isoginkgetin directly inhibits the chymotrypsin-like, trypsin-like, and caspase-like activities of the 20S proteasome. Isoginkgetin also is a general inhibitor of Pre-mRNA splicing.
S6851 RA-190 RA190, a bis-benzylidine piperidon, is a potent, selective and oral effective inhibitor of proteasome ubiquitin receptor RPN13/ADRM1 with anticancer activity. RA190 triggers ER stress response, p53/p21 signaling axis and autophagy in multiple myeloma cells.
S7038 Epoxomicin (BU-4061T) Epoxomicin (BU-4061T, Aids010837) 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. Epoxomicin promotes apoptosis.
Oxid Med Cell Longev, 2022, 2022:5044046
Neurosci Bull, 2022, 10.1007/s12264-022-00818-9
Cell Biol Toxicol, 2022, 10.1007/s10565-022-09699-0
S7049 Oprozomib (ONX 0912) Oprozomib (ONX 0912, PR-047) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM. Phase 1/2.
Mol Ther Nucleic Acids, 2022, 27:335-348
Pharmaceutics, 2021, 13(3)314
Autophagy, 2020, 10.1080/15548627.2020.1740529
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.
Oncol Rep, 2021, 45(4)34
Sci Rep, 2020, 10(1):15765
J Clin Pathol, 2020, jclinpath-2020-206618
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).
Nat Cell Biol, 2022, 24(3):364-372
Cancer Sci, 2020, 112(1):133-143
Oncol Rep, 2019, 41(5):2803-2817
S7504 Salinosporamide A (NPI-0052) Salinosporamide A (NPI-0052, ML858, Marizomib, MRZ) is a novel marine derived proteasome inhibitor which inhibits CT-L β5, C-L β1, and T-L β2 proteasome activities in human erythrocyte-derived 20S proteasomes with IC50 of 3.5 nM, 430 nM, 28 nM.
Mol Cancer Res, 2020, 18(7):1004-1017
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.
Autophagy, 2021, 1-19
Cancer Sci, 2020, 112(1):133-143
Sci Rep, 2018, 8(1):671
S8279 Shikonin (C.I. 75535) Shikonin (C.I. 75535, Anchusin, Anchusa acid, Alkanna Red, Isoarnebin 4, NSC 252844), a potent and specific Pyruvate kinase M2 (PKM2) inhibitor, is a major component of zicao (purple gromwell, the dried root of Lithospermum erythrorhizon), a Chinese herbal medicine with various biological activities. It is also an inhibitor of TMEM16A chloride channel activity using cell-based fluorescent-quenching assay. Shikonin exerts an anti-inflammatory effect by inhibiting tumor necrosis factor-α (TNF-α) and prevents activation of nuclear factor-κB (NF-κB) pathway via proteasome inhibition.
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Bioengineered, 2022, 13(3):5928-5941
S3269 Acetylcorynoline Acetylcorynoline, a major alkaloid component derived from Corydalis bungeana which is a traditional Chinese medical herb, shows anti-inflammatory properties. Acetylcorynoline may decrease egl-1 expression to suppress apoptosis pathways and increase rpn5 expression to enhance the activity of proteasomes.
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