-
MMP inhibitor
Marimastat acted as a broad-spectrum matrix metalloproteinase inhibitor.- Abdel-Aziz S Shatat, .et al. , Purinergic Signal, 2024, May 27 PMID: 38801618
- Kai Zhang, .et al. , Pharmaceutics, 2021, Nov 23;13(12):1990 PMID: 34959271
- Lv Y, .et al. , ACS Nano, 2018, Feb 27;12(2):1519-1536 PMID: 29350904
- ChaoQin, .et al. , Powder Technol, 2018, In Press
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Proteasome inhibitor
PR-171 (Carfilzomib) is a tetrapeptide epoxyketone and a selective proteasome inhibitor. It is an analog of epoxomicin.- Alireza Saedi, .et al. , J Prev Complement Med, 2025, 4(1): 26-34
- 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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HCV Nucleoside Inhibitor
PSI-6130(R 1656) is a Hepatitis C Virus Nucleoside Inhibitor.- Amitava Adhikary, .et al. , J Am Chem Soc., 2014, 136(44): 15646-15653 PMID: 25296262
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Caspase inhibitor
Q-VD-OPH is a selective, brain and cell permeable, highly potent and irreversible inhibitor of caspase-3 ( IC50=25nm), caspase-1 (IC50=50nM), caspase-8 (IC50=100nM) and caspase-9 (IC50=430nM).- Baosen Jia, .et al. , Nature, 2026, Apr;652(8112):1362-1374 PMID: 42020739
- Andrew Kent, .et al. , Nat Immunol, 2025, Jan;26(1):53-67 PMID: 39747433
- Anna L Koessinger, .et al. , Cell Death Differ, 2022, Apr 26 PMID: 35473984
- Florian J Bock, .et al. , Nat Commun, 2021, Nov 12;12(1):6572 PMID: 34772930
- Davide Pradella, .et al. , Nat Commun, 2021, 12: 4872 PMID: 34381052
- Haschka MD, .et al. , Cell Death Differ, 2020, Feb 3 PMID: 32015503
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Calpain Inhibitor III
MDL 28170 is a cell permeable selective inhibitor of Calpain 1, a Ca2+-dependent cysteine protease which has been implicated in apoptosis of immune cells as well as neuronal cells.- Barker BS, .et al. , Neuroscience, 2019, Nov 26. pii: S0306-4522(19)30796-1 PMID: 31783100
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Glutaminase inhibitor
CB-839 an is orally bioavailable inhibitor of glutaminase, with potential antineoplastic activity. CB-839 (Telaglenastat) also inudces autophagy and has antitumor activity.
- Beatriz Giesen, .et al. , Pharmaceutics, 2021, Feb 23;13(2):295 PMID: 33672398
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Caspase-1 inhibitor
Z-YVAD-FMK is a potent cell-permeable and irreversible inhibitor of caspase-1.- Binjie Yan, .et al. , Cell Death Discov, 2023, 9: 456 PMID: 38097554
- Yuping Fan, .et al. , Sci Transl Med, 2021, Jul 28;13(604):eabb1069 PMID: 34321317
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serine protease inhibitor
AEBSF HCl is a broad spectrum, irreversible serine protease inhibitor.- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
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DPP-IV Inhibitor
Vildagliptin is a dipeptidyl peptidase-4 (CD26) inhibitor.- Cecilia Villegas-Novoa, .et al. , Anal Chem, 2022, 94(27):9648-9655 PMID: 35758929
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γ-secretase inhibitor
BMS 299897 is an orally active, potent γ-secretase inhibitor (IC50 = 12 nM). Inhibits Aβ40 and Aβ42 formation in vitro (IC50 values are 7.4 and 7.9 nM respectively) and reduces Aβ in the brain, plasma and cerebrospinal fluid in vivo.- Chao Liu, .et al. , Cell Death Differ, 2018, Apr; 25(4): 661-676 PMID: 29238071
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neutrophil elastase inhibitor
Avelestat, also known as AZD9668, is a novel, oral inhibitor of neutrophil elastase (NE).- Chen Yang, .et al. , mBio, 2024, Oct 16;15(10):e0213024 PMID: 39287443
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HCV replication Inhibitor
Anguizole is a small molecule inhibits HCV replication and alters NS4B's subcellular distribution.- Choi M, .et al. , Virus Genes., 2013, Dec;47(3):395-407 PMID: 23868571
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NAE Inhibitor
NAE inhibitor MLN4924 binds to and inhibits NAE, which may result in the inhibition of tumor cell proliferation and survival.- Céline Moison, .et al. , EMBO Rep, 2025, Jun;26(11):2836-2854 PMID: 40295725
- Takumi Ito, .et al. , Research Square, 2023, 2023
- Blue-leaf A. Cordes, .et al. , Cancers (Basel), 2023, Mar; 15(6): 1846 PMID: 36980731
- Min Dong, .et al. , J Immunother Cancer, 2022, Oct;10(10):e005270 PMID: 36198437
- Corentin Mallet, .et al. , J Virol, 2021, Dec 22;JVI0142721 PMID: 34936483
- Nobuyuki Shimizu, .et al. , Commun Biol, 2021, Nov 11;4(1):1277 PMID: 34764413
- Jalila Chagraoui, .et al. , Cell Stem Cell, 2021, Jan 7;28(1):48-62.e6 PMID: 33417871
- Stephan Riesenberg, .et al. , Nat Commun, 2018, 9: 2164 PMID: 29867139
- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Richard J. Kraus, .et al. , PLoS Pathog, 2017, Jun; 13(6): e1006404 PMID: 28617871
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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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Hepatitis C virus NS3/4a protease inhibitor
Grazoprevir (MK-5172) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.- Deqiang Kong, .et al. , Nat Commun, 2024, Jun 8;15(1):4894 PMID: 38849338
- Xinyi Wang, .et al. , Nat Chem Biol, 2023, Oct 23 PMID: 37872400
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HCV NS3/4A protease inhibitor
Danoprevir is a potent inhibitor of the HCV NS3/4A serine protease.- Deqiang Kong, .et al. , Nat Commun, 2024, Jun 8;15(1):4894 PMID: 38849338
- Xinyi Wang, .et al. , Nat Chem Biol, 2023, Oct 23 PMID: 37872400
- Mahim Khan, .et al. , BMC Complement Med Ther, 2022, Apr 2;22(1):98 PMID: 35366855
- Inês GARCEZ PALHA, .et al. , Biol Open, 2018, Nov 7 PMID: 30404898
- Hui Shen, .et al. , PLoS One., 2013, 8(12): e82299 PMID: 24358168
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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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HIV Protease Inhibitor
Saquinavir is a protease inhibitor. Proteases are enzymes that cleave protein molecules into smaller fragments. Saquinavir inhibits both HIV-1 and HIV-2 proteases.- Ernawati Arifin Giri-Rachman, .et al. , ACS Synth Biol, 2024, Feb 16; 13(2): 509-520 PMID: 38316139
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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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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DPP-4 Inhibitor
Linagliptin is a DPP-4 inhibitor, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP).- Fen Zhuge, .et al. , Exp Neurol, 2024, Mar:373:114689 PMID: 38199510
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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).- Gideon Ong, .et al. , ResearchSquare, 2026, April 21st
- Melissa Campos, .et al. , Nat Metab, 2026, Feb;8(2):489-505 PMID: 41735679
- Ching-Chung Ko, .et al. , J Cancer, 2025, Nov 5;16(15):4408-4414 PMID: 41323782
- 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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Cathepsin S inhibitor
Z-FL-COCHO (LY3000328) is a novel Cathepsin S inhibitor.
- Gil-Im Mun, .et al. , Biochim Biophys Acta Mol Basis Dis, 2024, Sep 25;1871(1):167523 PMID: 39332782
- Fu R, .et al. , Sci Rep, 2020, Jan 29;10(1):1455 PMID: 31996771
- Klinngam W, .et al. , Sci Rep, 2019, Jul 2;9(1):9559 PMID: 31267034
- Chen CY, .et al. , Clin Sci (Lond), 2018, Oct 29;132(20):2221-2239 PMID: 30287519
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Gamma secretase inhibitor
LY-411575 is a selective, cell permeable, small molecule gamma secretase inhibitor.
- Haiwen Yu, .et al. , Immunol Invest, 2023, Feb;52(2):241-255 PMID: 36562737
- Wojciech J Szlachcic, .et al. , iScience, 2022, Jul 15;25(7) PMID: 35756892
- Zhang ZH, .et al. , APMIS, 2019, Jul 5 PMID: 31274210
- Bo Pang, .et al. , Biosci Rep, 2018, Dec 21; 38(6): BSR20181922 PMID: 30473538
- Shuo Li, .et al. , Int Immunopharmacol, 2018, Oct;63:129-136 PMID: 30086535
- Jiang BC, .et al. , Viral Immunol, 2017, Sep;30(7):522-532 PMID: 28410452
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HCV Polymerase Inhibitor
VCH-759 is a non-nucleoside inhibitor of HCV RNA-dependent polymerase with sub-micromolar IC50 values versus genotype 1a/1b replicons.- Hassan GS, .et al. , Eur J Med Chem, 2019, Oct 1;184:111747 PMID: 31604164
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Gamma-secretase inhibitor
RO4929097 is an orally bioavailable, small-molecule gamma secretase (GS) inhibitor with an IC50 of 4 nM.- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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Non-peptide calpain inhibitor
PD 150606 is a cell-permeable, non-competitive, selective, non-peptide Ca2+ dependent calpain inhibitor for calpain-1 and for calpain-2 directed towards the Ca2+ binding sites of calpain.- Hisamatsu Y, .et al. , Bioconjug Chem, 2017, Feb 15;28(2):507-523 PMID: 28032992
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Caspase-3 inhibitor
Z-DQMD-FMK is a synthetic peptide that irreversibly inhibits the activity of Caspase-3.- Jason Segura, .et al. , PLoS One, 2023, Feb 13;18(2):e0281087 PMID: 36780482
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caspase 8 inhibitor
Z-IETD-FMK is a specific inhibitor of caspase 8.- Jason Segura, .et al. , PLoS One, 2023, Feb 13;18(2):e0281087 PMID: 36780482
- Liqun Zhao, .et al. , Apoptosis, 2021, Apr 27 PMID: 33905036
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Caspase-9 Inhibitor
Z-LEHD-FMK is a synthetic peptide that irreversibly inhibits caspase-9 and related caspase activity.- Jason Segura, .et al. , PLoS One, 2023, Feb 13;18(2):e0281087 PMID: 36780482
- Wenquan Liang, .et al. , Sci Rep, 2016, 6: 38267 PMID: 27905569
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ADAM10 metalloprotease inhibitor
GI 254023X is a selective ADAM10 metalloprotease inhibitor; displays over 100-fold higher potency at ADAM10 compared to ADAM17.- Joanna Ireland, .et al. , Front Microbiol, 2024, Mar 20:15:1385775 PMID: 38572241
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HIV-1 protease inhibitor
Nelfinavir is a potent and orally bioavailable human immunodeficiency virus HIV-1 protease inhibitor (Ki=2 nM) and is widely prescribed in combination with HIV reverse transcriptase inhibitors for the treatment of HIV infection.- Joanna Ireland, .et al. , Front Microbiol, 2024, Mar 20:15:1385775 PMID: 38572241
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Yang PM, .et al. , Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
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MTP inhibitor
Lomitapide is a potent microsomal triglyceride transfer protein (MTP) inhibitor.- Julien Allard, .et al. , Cell Biol Toxicol, 2020, Jun 14 PMID: 32535746
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DPP-4 inhibitor
Trelagliptin is a highly selective, long-acting DPP-4 inhibitor.- Ki-Young Kim, .et al. , Pharmaceutics, 2024, Jan 13;16(1):106 PMID: 38258116
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DPP4 inhibitor
Gemigliptin is a highly selective dipeptidyl peptidase 4 (DPP4) inhibitor with a KD of 7.25 nM.- Ki-Young Kim, .et al. , Pharmaceutics, 2024, Jan 13;16(1):106 PMID: 38258116
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DPP-4 Inhibitor
Saxagliptin (BMS-477118) is a new dipeptidyl peptidase-4 (DPP-4) inhibitor with IC50 of 50 nM.- Ki-Young Kim, .et al. , Pharmaceutics, 2024, Jan 13;16(1):106 PMID: 38258116
- OHE El-Shoubashy, .et al. , JPC, 2020, 33, 59-70
- Sato T, .et al. , Sci Rep, 2019, Dec 2;9(1):18094 PMID: 31792328
- Chintan N. Koyani, .et al. , Front Physiol, 2018, 9: 1622 PMID: 30487758
- Koyani CN, .et al. , Biochem Pharmacol, 2016, Dec 1;145:64-80 PMID: 28859968
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MT1-MMP inhibitor
NSC-405020 is a membrane type-1 matrix metalloproteinase (MT1-MMP) inhibitor (IC50 > 100 μmol/L).- Kittaka M, .et al. , J Bone Miner Res, 2018, Jan;33(1):167-181 PMID: 28914985
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cathepsin inhibitor
VBY-825 is a novel, reversible cathepsin inhibitor with high potency against cathepsins B, L, S and V.- Laura Odongo, .et al. , Microbiol Spectr, 2023, Sep 20;11(5):e0190823 PMID: 37728342
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HCV NS3 protease Inhibitor
Ciluprevir is a specific and potent peptidomimetic inhibitor of the HCV NS3 protease.- Mahim Khan, .et al. , BMC Complement Med Ther, 2022, Apr 2;22(1):98 PMID: 35366855
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HCV NS3-4A protease inhibitor
Telaprevir (VX-950) is known as protease inhibitors that inhibits the hepatitis C virus NS3.4A serine protease.- Mahim Khan, .et al. , BMC Complement Med Ther, 2022, Apr 2;22(1):98 PMID: 35366855
- Adita Ayu Permanasari, .et al. , BMC Complement Med Ther, 2021, Oct 12;21(1):260 PMID: 34641875
- Che C Colpitts, .et al. , eLife, 2020, 9: e52237 PMID: 32539931
- TS Wahyuni, .et al. , Southeast Asian J Trop Med public health, 2020, 51(1)
- Stefan Bittmann, .et al. , J Regen Biol Med, 2020, 2(2):1-3
- Wahyuni TS, .et al. , J Basic Clin Physiol Pharmacol, 2019, Dec 14 PMID: 31837259
- Jacobs CL, .et al. , Nat Methods, 2018, Jul;15(7):523-526 PMID: 29967496
- Apriyanto DR, .et al. , Jpn J Infect Dis, 2016, May 20;69(3):213-20 PMID: 26255732
- Mizuki Yamamoto, .et al. , Antimicrob Agents Chemother, 2016, Nov; 60(11): 6532-6539 PMID: 27550352
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NS3 protease inhibitor
Asunaprevir is an inhibitor of the viral enzyme serine protease NS3.- Mahim Khan, .et al. , BMC Complement Med Ther, 2022, Apr 2;22(1):98 PMID: 35366855
- Miyayama Y, .et al. , Microbiol Immunol, 2019, Dec 19 PMID: 31854467
- Kato N, .et al. , Arch Virol, 2019, Dec 12 PMID: 31832864
- Fay EJ, .et al. , J Virol, 2018, Fay EJ PMID: 30282710
- Bennie Lemmens, .et al. , Mol Cell, 2018, Jul 5; 71(1): 117-128.e3 PMID: 30008317
- Ueda Y, .et al. , Virus Res, 2017, May 2;235:37-48 PMID: 28322919
- Furihata T, .et al. , Int J Antimicrob Agents, 2015, Oct;46(4):381-8 PMID: 26163159
- Tomomi Furihata, .et al. , Antimicrob Agents Chemother, 2014, 58(8): 4555-4564 PMID: 24867984
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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 PMID: 37979441
- 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 PMID: 32937365
- 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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Cathepsin B inhibitor
CA-074 methyl ester is a cell-permeable analog of CA-074 that acts as an irreversible cathepsin B inhibitor. CA-074 methyl ester is reported to inhibit bone resorption in rodent models and shown to inhibit B16 melanoma cell invasion in vitro.- Maohuan Ran, .et al. , Ecotoxicol Environ Saf, 2026, May:316:120163 PMID: 42013791
- Qian Chu, .et al. , Food Chem Toxicol, 2021, Jan;147:111867 PMID: 33217525
- Ye Tao, .et al. , Chemosphere, 2020, Mar;242:124959 PMID: 31669990
- Ming Sun, .et al. , J Agric Food Chem, 2018, Nov 21;66(46):12376-12384 PMID: 30392375
- Xueyan Wu, .et al. , Food Chem Toxicol, 2017, Aug;106(Pt A):273-282 PMID: 28579546
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Caspase-3 Inhibitor
Z-DEVD-FMK is a specific, irreversible Caspase-3 inhibitor.- Megumi Andoh, .et al. , Nat Commun, 2025, Jan 22;16(1):918 PMID: 39843445
- Geoffrey Canet, .et al. , Res Sq, 2024, May 14:rs.3.rs-4384494 PMID: 38798432
- Roi Ankawa, .et al. , Dev Cell, 2021, Jul 12;56(13):1900-1916 PMID: 34197726
- Yosefzon Y, .et al. , Mol Cell, 2018, May 17;70(4):573-587.e4 PMID: 29775577
- Akashi E, .et al. , Oncol Rep, 2017, Jul;38(1):506-514 PMID: 28586026
- Wenquan Liang, .et al. , Sci Rep, 2016, 6: 38267 PMID: 27905569
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HIV-1 attachment inhibitor
BMS-663068 is an HIV-1 attachment inhibitor in development for the treatment of HIV-1 infection.- Min Li, .et al. , J Infect Dis, 2025, Jul 16:jiaf373
- Min Li, .et al. , Nat Commun, 2020, 11: 4051 PMID: 32792548
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HIV-1 maturation inhibitor
Bevirimat (MPC-4326, PA-457, YK-FH312) is a first-in-class HIV-1 maturation inhibitor that demonstrates high potency in cell culture and has shown clinical efficacy in HIV-1-infected patients.- Mingzhang Wang, .et al. , Nat Commun, 2017, 8: 1779 PMID: 29176596
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HCV Nucleotide Inhibitor
PSI-7977 is a phosphoramidate prodrug of PSI-7851, a nucleoside analog that, when phosphorylated, inhibits the RNA-dependent RNA polymerase of hepatitis C virus (EC50 = 92 nM).- Miyayama Y, .et al. , Microbiol Immunol, 2019, Dec 19 PMID: 31854467
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NS5A inhibitor
Ledipasvir is an inhibitor of the hepatitis C virus HCV NS5A protein- Miyayama Y, .et al. , Microbiol Immunol, 2019, Dec 19 PMID: 31854467
- Sayuri Nitta, .et al. , Scientific Reports, 2019, 9: 5722 PMID: 30952914
- Sayuri Nitta, .et al. , Sci Rep, 2016, 6: 34652 PMID: 27703205
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Cysteine Protease inhibitor
E-64d is an inhibitor of cathepsins B and L and it is lysosome and cell permeable.- Montserrat Llanses Martinez, .et al. , PLoS Biol, 2024, Dec 12;22(12):e3002930 PMID: 39666682
- Montserrat Llanses Martinez, .et al. , bioRxiv, 2024, January 14
- Jason J McDougall, .et al. , Mol Pain, 2021, 17 PMID: 34006144
- Paudel DB, .et al. , Virology, 2018, Nov;524:127-139 PMID: 30195250
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MMP inhibitor
Batimastat (BB-94) is a potent and synthetic inhibitor of a broad spectrum of matrix metalloproteinases (MMPs), including interstitial collagenase (IC50 = 3 nM), stromelysin (IC50 = 20 nM), Mr 72,000 type IV collagenase (IC50 = 4 nM), Mr 92,000 type IV collagenase (IC50 = 4 nM), and matrilysin (IC50 = 6 nM). It is a low-molecular-weight (MW = 478) and peptide-like collagen substrate analogue consisting of a peptide backbone and a hydroxamic acid group which bind to MMPs and the catalytically active zinc atom respectively.- Nicholas Balestrieri, .et al. , Skelet Muscle, 2025, Nov 17;15(1):31 PMID: 41250146
- Joanna Ireland, .et al. , Front Microbiol, 2024, Mar 20:15:1385775 PMID: 38572241
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Pan Caspase Inhibitor
Z-VAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor. Inhibits caspase processing and apoptosis induction in tumor cells in vitro (IC50 = 0.0015 - 5.8 mM). Active in vivo.- Perla Nafeh, .et al. , BMC Complement Med Ther, 2025, Aug 13;25(1):304 PMID: 40804627
- Cheng Chen, .et al. , Neurochem Res, 2025, Mar 18;50(2):122 PMID: 40100474
- Lara Ebbert, .et al. , Antioxidants (Basel), 2024, Jul; 13(7): 864 PMID: 39061932
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