Proteasome

Inhibitory Selectivity

Catalog No.	Inhibitor Name	Proteasome	20S proteasome
A10160	Bortezomib (PS-341)		****
A11043	MG-132	*
A11278	Carfilzomib (PR-171)	***
A10602	MLN9708		***
A10600	Ixazomib (MLN2238)		****
A12653	ONX-0914 (PR-957)		**
A14181	Oprozomib (ONX 0912)		**
A11145	Delanzomib (CEP-18770)		***
A10192	Celastrol		*
A13650	VR23	****
A14146	PI-1840		**
A12730	Epoxomicin

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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(R)-MG-132

Catalog No. A21980
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proteasome inhibitor

(R)-MG-132 ((S,R,S)-(-)-MG-132) is the enantiomer of MG-132. (R)-MG-132 is a proteasome inhibitor with weaker cell cytotoxicity than MG-132. (R)-MG-132 stereoisomer is a more potent proteasome inhibitor than MG-132. 了解更多

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Ixazomib citrate

Catalog No. A18017
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20S proteasome inhibitor

Ixazomib citrate (MLN9708) is a reversible inhibitor of the chymotrypsin-like proteolytic β5 site of the 20S proteasome with an IC50 of 3.4 nM and a Ki of 0.93 nM. 了解更多

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Proteasome-IN-1

Catalog No. A12254
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proteasome inhibitor

Proteasome-IN-1 is a proteasome inhibitor extracted from patent WO 2013142376 A1. 了解更多

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ML604440

Catalog No. A18826
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proteasome β1i (LMP2) subunit inhibitor

ML604440 is a potent, specific and cell permeable proteasome β1i (LMP2) subunit inhibitor. 了解更多

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VR23

Catalog No. A13650
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Proteasome 抑制剂?

VR23是一个小分子，可有效抑制胰蛋白酶样蛋白酶体（IC50 = 1 nM），胰凝乳蛋白酶样蛋白酶体（IC50 = 50-100 nM）和半胱天冬酶样蛋白酶体（IC50 = 3uM）的活性。了解更多

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Epoxomicin

Catalog No. A12730
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Proteasome 抑制剂

Epoxomicin是从放线菌中分离出来的一种有效的抗肿瘤药，被用作20S蛋白酶体的选择性和不可逆抑制剂。了解更多

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AM 114

Catalog No. A14922
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20S proteasome 抑制剂

AM 114是硼查尔酮的衍生物，是一种有效的蛋白酶体小分子抑制剂，可抑制20S蛋白酶体的胰凝乳蛋白酶样活性，其50％抑制浓度的IC50值约为1 uM，导致大量积累泛素化的p53和其他细胞蛋白在整个细胞中的表达，而不会显着破坏p53与鼠类double minutes 2（mdm2）蛋白的相互作用。了解更多

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MG-262

Catalog No. A12220
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Proteasome 抑制剂

MG-262一种硼酸肽，是一种有效的蛋白酶体抑制剂，它选择性地和可逆地抑制蛋白酶体的糜蛋白酶活性。了解更多

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MG-115

Catalog No. A11601
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Reversible Proteasome 抑制剂

MG-115是一种有效的，可逆的肽醛抑制剂，具有蛋白酶类胰凝乳蛋白酶样和胱天蛋白酶样活性。它诱导p53依赖性细胞凋亡。了解更多

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Clasto-Lactacystin b-lactone

Catalog No. A15427
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20S proteasome 抑制剂

Clasto-Lactacystin b-lactone被鉴定为乳酸的活性代谢产物，这是由于半胱氨酸的消除和反应性b-内酯的形成所致。了解更多

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Dihydroeponemycin

Catalog No. A14932
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Proteasome 抑制剂

Dihydroeponemycin是蛋白酶体和抗肿瘤剂的抑制剂。了解更多

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Aclacinomycin A

Catalog No. A14910
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20S proteasome 抑制剂

Aclacinomycin A是一种蒽环类药物，是20S蛋白酶体胰凝乳蛋白酶样活性的特异性抑制剂。了解更多

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Marizomib (NPI-0052, salinosporamide A)

Catalog No. A13853
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Proteasome 抑制剂

Marizomib (NPI-0052,salinosporamide A)是一种天然存在的salinosporamide，从海洋放线菌Salinospora tropica中分离出来，具有潜在的抗肿瘤活性。了解更多

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- Tarantelli C, .et al. PQR309 Is a Novel Dual PI3K/mTOR Inhibitor with Preclinical Antitumor Activity in Lymphomas as a Single Agent and in Combination Therapy, Clin Cancer Res, 2018, Jan 1;24(1):120-129 PMID: 29066507
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PI-1840

Catalog No. A14146
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reversible proteasome 抑制剂

PI-1840是一种具有抗肿瘤活性的新型非共价快速可逆蛋白酶体抑制剂。了解更多

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ONX 0912 (Oprozomib)

Catalog No. A14181
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Proteasome 抑制剂

ONX 0912 (Oprozomib)是一种三肽环氧酮，可抑制对常规和硼替佐米治疗耐药的MM细胞的生长并诱导其凋亡。了解更多

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PSI

Catalog No. A14048
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Proteasome 抑制剂

PSI是蛋白酶体抑制剂，其抑制蛋白酶体的胰凝乳蛋白酶样活性。了解更多

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Gliotoxin

Catalog No. A13711
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20S proteasome 抑制剂

Gliotoxin是由曲霉菌和其他真菌的致病菌株产生的一种免疫抑制性真菌毒素。了解更多

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Lactacystin

Catalog No. A12768
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proteasome 抑制剂

Lactacystin是一种细胞可渗透的，有效的和选择性的蛋白酶体抑制剂。了解更多

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ONX-0914

Catalog No. A12653
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Immunoproteasome 抑制剂

ONX 0914是有效，选择性的免疫蛋白酶体亚基LMP7的抑制剂，在自身免疫性疾病（如类风湿性关节炎，炎性肠病和狼疮）中具有潜在的治疗应用。ONX 0914被设计为一种有效的免疫蛋白酶抑制剂，对组成型蛋白酶体的交叉反应最小。了解更多

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- Yuki Sasaki, .et al. Blockade of the CXCR3/CXCL10 axis ameliorates inflammation caused by immunoproteasome dysfunction, JCI Insight, 2022, Apr 8;7(7) PMID: 35393946
- Ming-Shu Mo, .et al. Dopaminergic neurons show increased low-molecular-mass protein 7 activity induced by 6-hydroxydopamine in vitro and in vivo, Transl Neurodegener, 2018, 7: 19 PMID: 30128145
- Ohkusu-Tsukada K, .et al. The Role of Proteasome Inhibitor MG132 in 2,4-Dinitrofluorobenzene-Induced Atopic Dermatitis in NC/Nga Mice, Int Arch Allergy Immunol, 2018, 176(2):91-100 PMID: 29669333
- Arimochi H, .et al. Differentiation of preadipocytes and mature adipocytes requires PSMB8, Sci Rep, 2016, May 26;6:26791 PMID: 27225296
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PR-171 (Carfilzomib)

Catalog No. A11278
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Proteasome 抑制剂

PR-171 (Carfilzomib)是四肽环氧酮和选择性蛋白酶体抑制剂。它是环氧霉素的类似物。了解更多

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- Ori Kalid, .et al. PTX80, A Novel Compound Targeting the Autophagy Receptor p62/SQSTM1 for Treatment of Cancer, Chem Biol Drug Des, 2022, Mar 24 PMID: 35322538
- Abbas Rahdar, .et al. Pluronic F127/carfilzomib-based nanomicelles as promising nanocarriers: synthesis, characterization, biological, and in silico evaluations, Journal of Molecular Liquids, 2022, 346: 118271
- Sadegh Zarei, .et al. Carfilzomib Induces Drug Resistance in A2780 Ovarian Cancer Cells Through p53-Dependent and Caspase-3 Independent Pathways, J Appl Biotechnol Rep, 2019, June;6(2):45-49
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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CEP-18770 (Delanzomib)

Catalog No. A11145
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Proteasome 抑制剂

CEP-18770 (Delanzomib)是一种新型口服活性蛋白酶体抑制剂，IC50为3.8 nM，具有良好的肿瘤选择性，可用于治疗对蛋白酶体抑制有反应的MM和其他恶性肿瘤。了解更多

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MLN2238 (Ixazomib)

Catalog No. A10600
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Proteasome 抑制剂

MLN2238 (Ixazomib)是20S蛋白酶体抑制剂的有效可逆特异性β5位点，IC50值为3.4 nM。了解更多

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MG-132

Catalog No. A11043
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Proteasome 抑制剂

MG-132是蛋白酶体（IC50 = 100 nM）和钙蛋白酶（IC50 = 1.2μM）的有效的细胞渗透抑制剂。了解更多

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- Vo Thi Anh Nguyet, .et al. Acquired resistance to severe ethanol stress-induced inhibition of proteasomal proteolysis in Saccharomyces cerevisiae, Biochim Biophys Acta Gen Subj, 2022, Sep 6;1866(12):130241 PMID: 36075516
- Jalila Chagraoui, .et al. UM171 Preserves Epigenetic Marks that Are Reduced in Ex Vivo Culture of Human HSCs via Potentiation of the CLR3-KBTBD4 Complex, Cell Stem Cell, 2021, Jan 7;28(1):48-62.e6 PMID: 33417871
- Eunsu Yoo, .et al. Anti-proliferative activity of A. Oxyphylla and its bioactive constituent nootkatone in colorectal cancer cells, BMC Cancer, 2020, Sep 14;20(1):881 PMID: 32928152
- Hua Xu, .et al. Preclinical Study Using ABT263 to Increase Enzalutamide Sensitivity to Suppress Prostate Cancer Progression Via Targeting BCL2/ROS/USP26 Axis Through Altering ARv7 Protein Degradation, Cancers (Basel), 2020, Apr; 12(4): 831 PMID: 32235588
- Chi-Hung R Or, .et al. Obatoclax, a Pan-BCL-2 Inhibitor, Downregulates Survivin to Induce Apoptosis in Human Colorectal Carcinoma Cells Via Suppressing WNT/β-catenin Signaling, Int J Mol Sci, 2020, Mar 5;21(5):1773 PMID: 32150830
- Ghosh S, .et al. Interactions between Viperin, Vesicle-Associated Membrane Protein A, and Hepatitis C Virus Protein NS5A Modulate Viperin Activity and NS5A Degradation, Biochemistry, 2020, Feb 18;59(6):780-789 PMID: 31977203
- Kondo H, .et al. PITHD1 is a proteasome-interacting protein essential for male fertilization, J Biol Chem, 2020, Feb 7;295(6):1658-1672 PMID: 31915251
- Ohigashi I, .et al. Trans-omics Impact of Thymoproteasome in Cortical Thymic Epithelial Cells, Cell Rep, 2019, Nov 26;29(9):2901-2916 PMID: 31775054
- Paudel DB, .et al. Expression and antiviral function of ARGONAUTE 2 in Nicotiana benthamiana plants infected with two isolates of tomato ringspot virus with varying degrees of virulence, Virology, 2018, Nov;524:127-139 PMID: 30195250
- Ohkusu-Tsukada K, .et al. The Role of Proteasome Inhibitor MG132 in 2,4-Dinitrofluorobenzene-Induced Atopic Dermatitis in NC/Nga Mice, Int Arch Allergy Immunol, 2018, 176(2):91-100 PMID: 29669333
- Chi-Hung R. Or, .et al. Obatoclax, a Pan-BCL-2 Inhibitor, Targets Cyclin D1 for Degradation to Induce Antiproliferation in Human Colorectal Carcinoma Cells, Int J Mol Sci, 2016, Jan; 18(1): 44 PMID: 28035994
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Bortezomib (Velcade)

Catalog No. A10160
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Proteasome 抑制剂

Bortezomib (Velcade)是26S蛋白酶体的高度选择性，可逆抑制剂。了解更多

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- Yoshitaka Sato, .et al. Epstein-Barr virus tegument protein BGLF2 in exosomes released from virus-producing cells facilitates de novo infection, Cell Commun Signal, 2022, Jun 21;20(1):95 PMID: 35729616
- Shin-Ichi Makino, .et al. Impairment of Proteasome Function in Podocytes Leads to CKD, J Am Soc Nephrol, 2021, Mar;32(3):597-613 PMID: 33510039
- Yusuke Yamashita, .et al. Targeting Adaptive IRE1α Signaling and PLK2 in Multiple Myeloma: Possible Anti-Tumor Mechanisms of KIRA8 and Nilotinib, Int J Mol Sci, 2020, Sep; 21(17): 6314 PMID: 32878237
- Nandini Verma, .et al. Synthetic lethal combination targeting BET uncovered intrinsic susceptibility of TNBC to ferroptosis, Sci Adv, 2020, 6 : eaba8968
- A Hayano, .et al. Cell-type-specific sensitivity of bortezomib in the methotrexate-resistant primary central nervous system lymphoma cells, Int J Clin Oncol, 2019, 1-10 PMID: 30993483
- Hiroshi Fukamachi, .et al. A subset of diffuse-type gastric cancer is susceptible to mTOR inhibitors and checkpoint inhibitors, J Exp Clin Cancer Res, 2019, 38:127 PMID: 30866995
- Y Sato, .et al. S-like phase CDKs stabilize the Epstein-Barr virus BDLF4 protein to temporally control late gene transcription, J Virol, 2019, Jan 30. pii: JVI.01707-18 PMID: 30700607
- Takashi Azuma, .et al. Removal of pharmaceuticals in water by introduction of ozonated microbubbles, SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Wenhan Deng, .et al. Variable Responses of MYC Translocation Positive Lymphoma Cell Lines To Different Combinations of Novel Agents: Impact of BCL2 Family Protein Expression, Transl Oncol, 2018, Oct; 11(5): 1147-1154 PMID: 30055346
- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Hokyung K. Chung, .et al. Tunable and reversible drug control of protein production via a self-excising degron, Nat Chem Biol, 2015, Sep; 11(9): 713-720 PMID: 26214256
- S Raz, .et al. Severe hypoxia induces complete antifolate resistance in carcinoma cells due to cell cycle arrest, Cell Death Dis., 2014, 5(2): e1067 PMID: 24556682
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MLN9708

Catalog No. A10602
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Proteasome 抑制剂

MLN9708是一种蛋白酶体抑制剂，可抑制蛋白酶体的活性，从而阻断通常由蛋白酶体进行的靶向蛋白水解。了解更多

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