Proteasome

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Proteasomeシグナル伝達経路

Proteasome製品

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  • Proteasome阻害剤 (17)
  • Proteasome活性剤(1)
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S2619 MG132 MG132 ((S,R,S)-(-)-MG132, Z-Leu-D-Leu-Leu-al) は、強力なプロテアソーム(ChTL、TL、PGPH) 阻害剤です。 MG132 はカルパイン (calpain) も阻害します (IC50 = 1.2 μM)。
Drug Resist Updat, 2024, 73:101063
Bioact Mater, 2024, 32:277-291
Nat Commun, 2024, 15(1):1642
S1013 Bortezomib ボルテゾミブ (Bortezomib (PS-341, LDP-341, MLM341, NSC 681239)) は強力な 20S プロテアソーム (20S proteasome) 阻害剤であり、Ki は 0.6 nM です。正常細胞に比べがん細胞に対してより高い選択性を示します。 ボルテゾミブ (PS-341) は NF-κB を阻害し ERK のリン酸化を誘導することにより、卵巣がんなどの固形腫瘍において カテプシンB (cathepsin B) を抑制し、オートファジー (autophagy) の分解過程を阻害します。
Cell Rep, 2024, 43(2):113769
J Transl Med, 2024, 22(1):208
J Med Chem, 2024, 67(1):572-585
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.
J Transl Med, 2024, 22(1):208
iScience, 2024, 27(2):109015.
Cell Discov, 2023, 9(1):47
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 Rep Med, 2023, 10.1016/j.xcrm.2023.101286
iScience, 2023, 26(8):107302
iScience, 2023, 26(8):107302
S8279 Shikonin Shikonin, 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.
J Pharm Anal, 2023, 13(2):187-200
Cancer Sci, 2023, 114(3):806-821
Cancers (Basel), 2023, 15(17)4356
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.
Viruses, 2023, 15(10)2001
Life Sci Alliance, 2023, 6(5)e202201726
Cancer Res, 2022, 82(20):3701-3717
S7049 Oprozomib Oprozomibが選択的に 20Sプロテアソーム β5/LMP7 のCT-Lの活性を阻害し、IC50 が 36 nM/82 nMです。
Biosci Rep, 2023, 43(1)BSR20222102
Microbiol Spectr, 2023, 11(5):e0190423
Microbiol Spectr, 2023, 10.1128/spectrum.01904-23
S1290 Celastrol Celastrol 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.
Redox Biol, 2023, 66:102845
Redox Biol, 2023, 66:102845
J Pharm Anal, 2023, 13(2):156-169
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.
RMD Open, 2023, 9(1)e002818
bioRxiv, 2023, 2023.09.15.557918
bioRxiv, 2023, 2023.09.15.557918
S1157 Delanzomib 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.
J Fungi (Basel), 2022, 8(2)92
Pharmaceutics, 2021, 13(3)314
Autophagy, 2020, 10.1080/15548627.2020.1740529
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.
J Exp Clin Cancer Res, 2022, 41(1):249
Cell Death Dis, 2022, 13(3):197
Front Pharmacol, 2022, 13:1032975
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.
Microbiol Spectr, 2023, 11(5):e0190423
Microbiol Spectr, 2023, 10.1128/spectrum.01904-23
Autophagy, 2021, 1-19
S7504 Marizomib (Salinosporamide A) Marizomib (Salinosporamide A) 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 Oncol, 2023, 17(9):1821-1843
Mol Oncol, 2023, 17(9):1821-1843
Microbiol Spectr, 2023, 11(5):e0190423
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.
iScience, 2023, 26(6):106997
J Dermatol Sci, 2022, S0923-1811(22)00125-6
PLoS One, 2022, 17(12:e0274704)
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, 10.3892/or.2019.7040
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.
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.
S2619 MG132 MG132 ((S,R,S)-(-)-MG132, Z-Leu-D-Leu-Leu-al) は、強力なプロテアソーム(ChTL、TL、PGPH) 阻害剤です。 MG132 はカルパイン (calpain) も阻害します (IC50 = 1.2 μM)。
Drug Resist Updat, 2024, 73:101063
Bioact Mater, 2024, 32:277-291
Nat Commun, 2024, 15(1):1642
S1013 Bortezomib ボルテゾミブ (Bortezomib (PS-341, LDP-341, MLM341, NSC 681239)) は強力な 20S プロテアソーム (20S proteasome) 阻害剤であり、Ki は 0.6 nM です。正常細胞に比べがん細胞に対してより高い選択性を示します。 ボルテゾミブ (PS-341) は NF-κB を阻害し ERK のリン酸化を誘導することにより、卵巣がんなどの固形腫瘍において カテプシンB (cathepsin B) を抑制し、オートファジー (autophagy) の分解過程を阻害します。
Cell Rep, 2024, 43(2):113769
J Transl Med, 2024, 22(1):208
J Med Chem, 2024, 67(1):572-585
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.
J Transl Med, 2024, 22(1):208
iScience, 2024, 27(2):109015.
Cell Discov, 2023, 9(1):47
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 Rep Med, 2023, 10.1016/j.xcrm.2023.101286
iScience, 2023, 26(8):107302
iScience, 2023, 26(8):107302
S8279 Shikonin Shikonin, 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.
J Pharm Anal, 2023, 13(2):187-200
Cancer Sci, 2023, 114(3):806-821
Cancers (Basel), 2023, 15(17)4356
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.
Viruses, 2023, 15(10)2001
Life Sci Alliance, 2023, 6(5)e202201726
Cancer Res, 2022, 82(20):3701-3717
S7049 Oprozomib Oprozomibが選択的に 20Sプロテアソーム β5/LMP7 のCT-Lの活性を阻害し、IC50 が 36 nM/82 nMです。
Biosci Rep, 2023, 43(1)BSR20222102
Microbiol Spectr, 2023, 11(5):e0190423
Microbiol Spectr, 2023, 10.1128/spectrum.01904-23
S1290 Celastrol Celastrol 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.
Redox Biol, 2023, 66:102845
Redox Biol, 2023, 66:102845
J Pharm Anal, 2023, 13(2):156-169
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.
RMD Open, 2023, 9(1)e002818
bioRxiv, 2023, 2023.09.15.557918
bioRxiv, 2023, 2023.09.15.557918
S1157 Delanzomib 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.
J Fungi (Basel), 2022, 8(2)92
Pharmaceutics, 2021, 13(3)314
Autophagy, 2020, 10.1080/15548627.2020.1740529
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.
J Exp Clin Cancer Res, 2022, 41(1):249
Cell Death Dis, 2022, 13(3):197
Front Pharmacol, 2022, 13:1032975
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.
Microbiol Spectr, 2023, 11(5):e0190423
Microbiol Spectr, 2023, 10.1128/spectrum.01904-23
Autophagy, 2021, 1-19
S7504 Marizomib (Salinosporamide A) Marizomib (Salinosporamide A) 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 Oncol, 2023, 17(9):1821-1843
Mol Oncol, 2023, 17(9):1821-1843
Microbiol Spectr, 2023, 11(5):e0190423
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.
iScience, 2023, 26(6):106997
J Dermatol Sci, 2022, S0923-1811(22)00125-6
PLoS One, 2022, 17(12:e0274704)
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, 10.3892/or.2019.7040
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.
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.

Proteasome阻害剤の選択性比較

Tags: Proteasome inhibition | ubiquitin-Proteasome system | ubiquitin-Proteasome pathway | Proteasome activity | Proteasome function | ubiquitin-Proteasome degradation | Proteasome assay | Proteasome structure | Proteasome purification | Proteasome inhibitors in cancer therapy | Proteasome cleavage | 20s Proteasome activity | 26s Proteasome structure | Proteasome inhibition assay | Proteasome inhibitor drugs | Proteasome inhibitor review | Proteasomal inhibitor | Proteasomal inhibitors