Catalog No.
Product Name
Application
Product Information
Citations
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Proteasome inhibitor
Bortezomib is a highly selective, reversible inhibitor of the 26S proteasome- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Yodita Asfaha, .et al. , Eur J Med Chem, 2024, 263: 115907
- Tomoyuki Abe, .et al. , Eur J Pharmacol, 2022, Nov 15;935:175321 PMID: 36228744
- Yoshitaka Sato, .et al. , Cell Commun Signal, 2022, Jun 21;20(1):95 PMID: 35729616
- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- Shin-Ichi Makino, .et al. , J Am Soc Nephrol, 2021, Mar;32(3):597-613 PMID: 33510039
- Yusuke Yamashita, .et al. , Int J Mol Sci, 2020, Sep; 21(17): 6314 PMID: 32878237
- Nandini Verma, .et al. , Sci Adv, 2020, 6 : eaba8968
- A Hayano, .et al. , Int J Clin Oncol, 2019, 1-10 PMID: 30993483
- Hiroshi Fukamachi, .et al. , J Exp Clin Cancer Res, 2019, 38:127 PMID: 30866995
- Y Sato, .et al. , J Virol, 2019, Jan 30. pii: JVI.01707-18 PMID: 30700607
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Wenhan Deng, .et al. , Transl Oncol, 2018, Oct; 11(5): 1147-1154 PMID: 30055346
- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Hokyung K. Chung, .et al. , Nat Chem Biol, 2015, Sep; 11(9): 713-720 PMID: 26214256
- S Raz, .et al. , Cell Death Dis., 2014, 5(2): e1067 PMID: 24556682
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Proteasome Inhibitor
MLN2238 is a potent reversible and specific β5 site of the 20S proteasome inhibitor with an IC50 value of 3.4 nM.- Suryalakshmi Pandurangan, .et al. , ACS Appl Bio Mater, 2025, Sep 15;8(9):7628-7639 PMID: 40778987
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Proteasome Inhibitor
Ixazomib Citrate (MLN9708) Analogue is a proteasome inhibitor, which inhibits the activity of the proteasome, blocking the targeted proteolysis normally performed by the proteasome.
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Proteasome inhibitor
MG-132 is a potent cell-permeable inhibitor of proteasome (IC50 = 100 nM) and calpain (IC50 = 1.2 μM).- Fasih A Rahman, .et al. , J Biomed Sci, 2025, Aug 19;32(1):77 PMID: 40830874
- Céline Moison, .et al. , EMBO Rep, 2025, Jun;26(11):2836-2854 PMID: 40295725
- Ravindra Pramod Deshpande, .et al. , EMBO Mol Med, 2025, Apr;17(4):797-822 PMID: 40087501
- Fasih A Rahman, .et al. , J Biomed Sci, 2025, Feb 18;32(1):29 PMID: 39979946
- Laurence J Seabrook, .et al. , Nat Chem Biol, 2024, Dec;20(12):1566-1576 PMID: 39414979
- Nathan Bulangalire, .et al. , Biochimie, 2024, Apr 16:S0300-9084(24)00079-8 PMID: 38636798
- Yao-Yu Hsieh, .et al. , Mol Oncol, 2023, Oct 16 PMID: 37842807
- Carolina N Franco, .et al. , Sci Adv, 2023, Sep 8;9(36):eadi2232 PMID: 37682999
- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- Vo Thi Anh Nguyet, .et al. , Biochim Biophys Acta Gen Subj, 2022, Sep 6;1866(12):130241 PMID: 36075516
- Jalila Chagraoui, .et al. , Cell Stem Cell, 2021, Jan 7;28(1):48-62.e6 PMID: 33417871
- Eunsu Yoo, .et al. , BMC Cancer, 2020, Sep 14;20(1):881 PMID: 32928152
- Hua Xu, .et al. , Cancers (Basel), 2020, Apr; 12(4): 831 PMID: 32235588
- Chi-Hung R Or, .et al. , Int J Mol Sci, 2020, Mar 5;21(5):1773 PMID: 32150830
- Ghosh S, .et al. , Biochemistry, 2020, Feb 18;59(6):780-789 PMID: 31977203
- Kondo H, .et al. , J Biol Chem, 2020, Feb 7;295(6):1658-1672 PMID: 31915251
- Ohigashi I, .et al. , Cell Rep, 2019, Nov 26;29(9):2901-2916 PMID: 31775054
- Paudel DB, .et al. , Virology, 2018, Nov;524:127-139 PMID: 30195250
- Ohkusu-Tsukada K, .et al. , Int Arch Allergy Immunol, 2018, 176(2):91-100 PMID: 29669333
- Chi-Hung R. Or, .et al. , Int J Mol Sci, 2016, Jan; 18(1): 44 PMID: 28035994
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Proteasome inhibitor
CEP-18770 is a novel orally active proteasome inhibitor with a favorable tumor selectivity profile for the treatment of MM and other malignancies responsive to proteasome inhibition. -
Proteasome inhibitor
PR-171 (Carfilzomib) is a tetrapeptide epoxyketone and a selective proteasome inhibitor. It is an analog of epoxomicin.- Mohammad Reza Hajinezhad, .et al. , Discov Nano, 2025, Aug 14;20(1):135 PMID: 40804566
- Zahra Mirzaei, .et al. , BMC Complement Med Ther, 2025, Jan 22;25(1):15 PMID: 39844241
- Andrew Thorne, .et al. , PLoS One, 2023, Jun 8;18(6):e0286783 PMID: 37289679
- Mahmood Barani, .et al. , J Drug Deliv Sci Technol, 2023, 81: 104268
- Ori Kalid, .et al. , Chem Biol Drug Des, 2022, Mar 24 PMID: 35322538
- Abbas Rahdar, .et al. , Journal of Molecular Liquids, 2022, 346: 118271
- Sadegh Zarei, .et al. , J Appl Biotechnol Rep, 2019, June;6(2):45-49
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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NF-kB inhibitor/Proteasome activator
18α-Glycyrrhetinic acid (18α-GA) is a bioactive triterpenoid found in licorice. It shows selective inhibition of 11-HSD1 (11-hydroxysteroid dehydrogenase 1). -
proteasome inhibitor
Proteasome-IN-1 is a proteasome inhibitor extracted from patent WO 2013142376 A1. -
Immunoproteasome inhibitor
ONX 0914 is an immunoproteasome inhibitor with potential treatment applications in autoimmune disorders, such as rheumatoid arthritis, inflammatory bowel disease and lupus. ONX 0914 was designed to be a potent inhibitor of the immunoproteasome with minimal cross-reactivity for the constitutive proteasome.- David J Zahavi, .et al. , Cancer Biol Ther, 2023, Dec 31;24(1):2269637 PMID: 37878417
- Yuki Sasaki, .et al. , JCI Insight, 2022, Apr 8;7(7) PMID: 35393946
- Ming-Shu Mo, .et al. , Transl Neurodegener, 2018, 7: 19 PMID: 30128145
- Ohkusu-Tsukada K, .et al. , Int Arch Allergy Immunol, 2018, 176(2):91-100 PMID: 29669333
- Arimochi H, .et al. , Sci Rep, 2016, May 26;6:26791 PMID: 27225296
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Proteasome inhibitor
Epoxomicin is a potent anti-tumor agent isolated from Actinomycetes that is used as a selective and irreversible inhibitor of the 20S proteasome.- F Cerruti, .et al. , Res Vet Sci, 2023, Sep;162:104950 PMID: 37453228
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proteasome inhibitor
Lactacystin is a cell-permeable, potent and selective proteasome inhibitor.- Duško Lainšček, .et al. , Cell Commun Signal, 2024, Nov 16;22(1):549 PMID: 39550582
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Proteasome Inhibitor
Marizomib is a naturally-occurring salinosporamide, isolated from the marine actinomycete Salinospora tropica, with potential antineoplastic activity.- Tarantelli C, .et al. , Clin Cancer Res, 2018, Jan 1;24(1):120-129 PMID: 29066507
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Proteasome inhibitor
ONX 0912 is a tripeptide epoxyketone, which inhibits growth and induces apoptosis in MM cells resistant to conventional and bortezomib therapies. -
20S proteasome inhibitor
Aclarubicin A, an anthracycline drug, specific inhibitor of the 20S proteasome chymotrypsin-like activity. -
20S proteasome inhibitor
AM 114, a derivative of boronic chalcone, is a potent small-molecule inhibitor of the proteasome that inhibits the chymotrypsin-like activity of the 20S proteasome, with a value of 50% inhibition concentration IC50 of approximately 1 uM, resulting in a significant accumulation of ubiquitinated p53 and other cellular proteins in whole cells without significantly disrupting the interaction of p53 and murine double minute 2 (mdm2) proteins. -
Proteasome inhibitor
Dihydroeponemycin is an inhibitor of proteasome and antitumor reagent. -
20S proteasome inhibitor
Clasto-lactacystin b-lactone was later identified as the active metabolite of lactacystin, resulting from the elimination of cysteine and the formation of a reactive b-lactone. -
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. -
alpains 1 and 2 inhibitor
Alicapistat (ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential use in the treatment of Alzheimer's disease (AD). -
proteasome subunit Rpn11 inhibitor
Rpn11-IN-1 (Capzimin intermediate) is a potent and selective inhibitor of proteasome subunit Rpn11 with an IC50 of 390 nM. -
chymotrypsin inhibitor
FK-448 Free base is an effective and specific inhibitor of chymotrypsin, with an IC50 of 720 nM. -
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. -
Proteasome Inhibitor
TP-110 is a selective proteasome inhibitor that targets the protease-like activity of the 20S proteasome, leaving trypsin-like and peptidyl-glutamyl peptide hydrolysis activities unaffected. This compound effectively disrupts the NF-κB signaling pathway, leading to activation of caspases 3, 8, and 9, and subsequent PARP cleavage, while decreasing levels of anti-apoptotic proteins cIAP-1 and XIAP. TP-110 induces G2/M phase cell cycle arrest and promotes apoptosis in cancer cells, making it a valuable tool for researching various malignancies, including prostate cancer and multiple myeloma. -
HDAC6/Proteasome Inhibitor
AMC-3-030 is a selective inhibitor targeting histone deacetylase 6 (HDAC6) and the chymotrypsin-like activity of the proteasome, demonstrating IC50 values of 884 nM and 4.17 nM, respectively. This compound exhibits a proliferative inhibitory effect and has been shown to reduce levels of α-tubulin and β-actin. AMC-3-030 serves as a valuable tool for investigating mechanisms related to multiple myeloma and other related research applications. -
Proteasome Inhibitor
Ub4ix is a potent proteasome inhibitor that selectively protects K48-linked ubiquitin chains from deubiquitinating enzymes (DUBs), thereby preventing the degradation of ubiquitin-tagged proteins. This compound has demonstrated significant biological activity, including the reduction of cell viability and induction of apoptosis in HeLa cells, with an IC50 value of 1.6 μM. Ub4ix is a valuable tool for research applications focused on understanding protein homeostasis and the role of the proteasome in cellular processes. -
Proteasome Inhibitor
Baceridin is a proteasome inhibitor characterized as a cyclic hexapeptide. Isolated from the culture medium of Epiphytic Bacillus, it disrupts proteasome function, leading to inhibition of cell cycle progression and induction of apoptosis in tumor cells via a p53-independent mechanism. This compound is valuable for cancer research applications, particularly in studies exploring proteasome inhibition and its effects on tumor biology. -
LonP1/ CT-L proteasome inhibitor
BT317 is a selective inhibitor of mitochondrial Lon peptidase I (LonP1) and the caspase-like (CT-L) activity of the proteasome. This compound has been shown to increase the production of reactive oxygen species (ROS), leading to apoptosis in astrocytoma cells. BT317 exhibits significant antitumor activity, making it a valuable reagent for research in cancer biology and therapeutic applications targeting gliomas. -
Proteasome Inhibitor
YSY01A is a potent proteasome inhibitor that promotes apoptosis in cancer cells, demonstrating IC50 values of 51.0 nM in HEK293T, 9.2 nM in A549, 5.2 nM in MCF-7, 8.9 nM in MGC-803, and 35.4 nM in PC-3M cell lines. This compound effectively disrupts constitutive STAT3 signaling by downregulating gp130 and JAK2 in human A549 lung cancer cells. YSY01A serves as a valuable tool for research in cancer therapy and apoptosis mechanisms. -
Proteasome Inhibitor
CEP1612 is a dipeptidyl proteasome inhibitor that exhibits an IC50 of 60 nM. This compound induces the expression of cell cycle regulators p21(WAF1) and p27(KIP1), leading to enhanced apoptotic activity in cancer cells. Due to its ability to disrupt proteasomal degradation, CEP1612 demonstrates significant anticancer efficacy in vivo, making it a valuable tool for research into cancer therapeutics. -
Proteasome Inhibitor
NIC-0102 is an orally active proteasome inhibitor that specifically targets NLRP3 inflammatory vesicle activation, exhibiting a pIC50 of 7.55. This compound demonstrates significant anti-inflammatory effects in models of dextran sulfate sodium (DSS)-induced ulcerative colitis. Additionally, NIC-0102 is effective in inhibiting the production of pro-IL-1β, making it a valuable tool for research in inflammation and related pathways. -
Proteasome Inhibitor
UR238 is a potent proteasome inhibitor that decreases the levels of the immunomodulatory protein HE4. Additionally, UR238 effectively reduces PDL1 expression on various cell types. Its anticancer properties make it a valuable reagent for research focusing on epithelial ovarian cancer. -
20S proteasome Inhibitor
BSc2118 is a potent inhibitor of the 20S proteasome, exhibiting an IC50 of approximately 50 nM. This compound induces G2/M phase cell cycle arrest and apoptosis in myeloma cells while inhibiting cytoprotective autophagy and tumor angiogenesis. Additionally, BSc2118 reduces matrix metalloproteinase 9 (MMP9) activity, promotes angioneurogenesis, and mitigates cerebral toxicity associated with recombinant tissue-type plasminogen activator. Its applications are relevant in the studies of cerebral ischemia and multiple myeloma. -
Dopamine receptor Agonist, 20S proteasome Activator
Apomorphine hydrochloride is a potent dopamine receptor agonist and a known activator of the 20S proteasome. It enhances proteasomal and insulin-degrading enzyme activities, facilitating the degradation of intracellular amyloid-beta (Aβ), phosphorylated tau (p-tau), and p53, thereby reducing their levels in neuronal cells. This compound is particularly relevant for research focused on neurodegenerative disorders such as Alzheimer's disease and psychiatric conditions including schizophrenia. -
Proteasome Inhibitor
Antitrypanosomal agent 15 is a selective proteasome inhibitor targeting Trypanosoma cruzi, with an impressive pIC50 of 7.4 for the T. cruzi proteasome and minimal activity (pIC50 < 4) against human proteasomes. This orally active compound demonstrates excellent brain penetration and favorable ADME properties, making it suitable for research focused on Chagas disease and related therapeutic interventions. Its selectivity and efficacy highlight its potential for advancing studies in trypanosomiasis. -
20S Proteasome Inhibitor
20S Proteasome-IN-4 is a selective inhibitor of the 20S proteasome, exhibiting an IC50 of 6.3 nM against Trypanosoma brucei brucei. This brain-penetrant compound is orally active and demonstrates potential for research into human African trypanosomiasis (HAT). Its specificity for the parasite makes it a valuable tool for studying proteasomal functions in this significant infectious disease.
