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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
- Rushikesh Deshpande, .et al. , Int J Mol Sci, 2024, Jan 18;25(2):1157 PMID: 38256231
- Sarah Metcalfe, .et al. , J Leukoc Biol, 2023, Jul 27;qiad089 PMID: 37497744
- Kazutoshi Toriyama, .et al. , Oncol Lett, 2023, Nov 10;27(1):12 PMID: 38028184
- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Akira Endo, .et al. , Dev Cell, 2023, Oct 9;58(19):1819-1829 PMID: 37716356
- Rui Zhou, .et al. , Nagoya J Med Sci, 2023, Aug;85(3):579-591 PMID: 37829490
- Chantal-Kristin Wenzel, .et al. , Toxicol In Vitro, 2023, Sep;91:105625 PMID: 37268255
- Joshua H Choe, .et al. , Cancer Discov, 2023, May 4;13(5):1250-1273 PMID: 37067901
- Yu-Chih Hsu, .et al. , Int J Med Sci, 2023, 20(4): 444-454 PMID: 37057216
- Debin Qi, .et al. , Cell Cycle, 2023, Apr;22(7):818-828 PMID: 36482709
- Ming-Chun Hung, .et al. , Cell Biosci, 2022, 12: 122 PMID: 35918763
- Kaori Kanemaru, .et al. , Nat Commun, 2022, May 9;13(1):2347 PMID: 35534464
- Chie Ishikawa, .et al. , Invest New Drugs, 2022, Aug;40(4):718-727 PMID: 35477814
- Aida Falgas, .et al. , Biomed Pharmacother, 2022, Jun;150:112940 PMID: 35421785
- Sumire Suzuki, .et al. , Oncol Rep, 2022, Feb;47(2):40 PMID: 34958115
- Lina Y Abou Zeid, .et al. , Cell Stress Chaperones, 2022, Jan;27(1):11-25 PMID: 34719748
- Simon Boudreault, .et al. , Viruses, 2022, Dec 3;14(12):2710 PMID: 36560714
- Kosar Jabbari, .et al. , Cancers (Basel), 2021, Sep 8;13(18):4521 PMID: 34572749
- Xiaoyue Deng, .et al. , Invest Ophthalmol Vis Sci, 2021, May 3;62(6):1 PMID: 33938913
- Liqun Zhao, .et al. , Apoptosis, 2021, Apr 27 PMID: 33905036
- Sofia Giacosa, .et al. , Cancers (Basel), 2021, Feb 2;13(3):576 PMID: 33540838
- Hideyuki Kinoshita, .et al. , Anticancer Res, 2021, Dec;41(12):6013-6021 PMID: 34848455
- Hannes Schmid, .et al. , Haematologica, 2021, Jan 14 PMID: 33440919
- Hideyuki Kinoshita, .et al. , Anticancer Res, 2021, Oct;41(10):4947-4955 PMID: 34593442
- Hua Xu, .et al. , Cancers (Basel), 2020, Apr; 12(4): 831 PMID: 32235588
- El-Ashmawy NE, .et al. , Pathol Oncol Res, 2020, Jan 4 PMID: 31902118
- Schneider D, .et al. , Clin Epigenetics, 2019, Jul 2;11(1):98 PMID: 31266541
- Fujiki K, .et al. , Cell Death Differ, 2019, Feb 25 PMID: 30804470
- T Yamamoto, .et al. , Cell Microbiol, 2019, 2019 PMID: 30702185
- Maeda N, .et al. , J Biol Chem, 2019, Nov 13. pii: jbc.RA119.010379 PMID: 31723031
- Miyazawa S, .et al. , Breast Cancer, 2019, Oct 17 PMID: 31625014
- Yeh HT, .et al. , Eur J Pharmacol, 2019, Sep 10;863:172658 PMID: 31518562
- D. Bosc, .et al. , Sci Rep, 2018, 8: 11653 PMID: 30076329
- Tsukamoto H, .et al. , J Biol Chem, 2018, Jun 29;293(26):10186-10201 PMID: 29760187
- Hiroshi Kuribayashi, .et al. , Cell Death Dis, 2018, Sep; 9(9): 891 PMID: 30166529
- Matsuo J, .et al. , Can J Microbiol, 2018, Oct 18:1-9 PMID: 30336068
- Orly Ravid, .et al. , Front Cell Neurosci, 2018, 12: 359 PMID: 30459557
- Im E, .et al. , Life Sci, 2018, Sep 15;209:259-266 PMID: 30107166
- Szalai P, .et al. , Cell Calcium, 2018, Dec;76:48-61 PMID: 30261424
- Im E, .et al. , Life Sci, 2018, Jan 1;192:286-292 PMID: 29128513
- Iriyama N, .et al. , Leuk Lymphoma, 2018, Jun;59(6):1439-1450 PMID: 28918692
- Birte Plitzko, .et al. , J Biol Chem, 2017, Dec 22; 292(51): 21102-21116 PMID: 29074620
- Akashi E, .et al. , Oncol Rep, 2017, Jul;38(1):506-514 PMID: 28586026
- Amprenavir is an human immunodeficiency virus (HIV) protease inhibitor with IC50 of 14.6 ?? 12.5 ng/ml for wild-type HIV isolates
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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Neutrophil elastase inhibitor
Sivelestat sodium salt is a selective leukocyte elastase inhibitor (IC50 = 44 nM) that displays no activity at a range of other proteases. It inhibits NF-kB activation and LTB4-induced neutrophil transmigration in vitro.- Shasha He, .et al. , Nature Biomedical Engineering, 2023, 7: 281-297 PMID: 36941352
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NS5A inhibitor
BMS-790052 is an NS5A inhibitor under investigation for the treatment of hepatitis C virus (HCV) infection.- Shirasaki T, .et al. , Hepatology., 2014, 60(5):1519-30 PMID: 24962339
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Caspase inhibitor
Nivocasan is a novel caspase-inhibitor has demonstrated hepatoprotective activity in fibrosis/apoptosis animal models.- Sohya Fujimoto, .et al. , Cells, 2025, Mar 27;14(7):498 PMID: 40214452
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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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Gamma-secretase inhibitor
FLI-06 is a Notch inhibitor and the early secretory pathway inhibitor. FLI-06 disrupts the Golgi apparatus in a manner distinct from that of brefeldin A and golgicide A.- Tan YJ, .et al. , Future Med Chem, 2018, Sep 1;10(17):2039-2057 PMID: 30066578
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Thrombin inhibitor
BIBR 953 (Dabigatran, Pradaxa) is a highly selective, reversible, and potent thrombin inhibitor and is orally available as the prodrug, dabigatran etexilate. It has shown antithrombotic efficacy in animal models of thrombosis, with a rapid onset of action and predictable pharmacodynamic response.
- Tanaka M, .et al. , J Pharmacol Sci, 2016, Jul;131(3):162-71 PMID: 27426918
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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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Cathepsin B inhibitor
CA-074 is a potent inhibitor of cathepsin B with a Ki of 2 to 5 nM.- Tianming Qiu, .et al. , Cell Death Dis, 2018, Oct; 9(10): 946 PMID: 30237538
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ADAM17 inhibitor
KP-457 is a selective a disintegrin and metalloproteinase 17 (ADAM17) inhibitor, with higher selectivity for ADAM17 than for other MMPs and ADAM10, and IC50s are 11.1 nM (ADAM17), 748 nM (ADAM10), 717 nM (MMP2), 9760 nM (MMP3), 2200 nM (MMP8), 5410 nM (MMP9), 930 nM (MMP13), 2140 nM (MMP14), and 7100 nM (MMP17), respectively.- Tolulope E Ayo, .et al. , Cell Signal, 2023, May;105:110607 PMID: 36690134
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HCV NS5A inhibitor
BMS-790052 is an NS5A inhibitor under investigation for the treatment of hepatitis C virus (HCV) infection.- TS Wahyuni, .et al. , Southeast Asian J Trop Med public health, 2020, 51(1)
- Miyayama Y, .et al. , Microbiol Immunol, 2019, Dec 19 PMID: 31854467
- Sato K, .et al. , Hepatol Res, 2018, Feb;48(3):E347-E353 PMID: 28834004
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Gamma secretase inhibitor
DAPT (GSI-IX) is an inhibitor of γ-secretase that causes a reduction in Aβ40 and Aβ42 levels in human primary neuronal cultures with IC50 values of 115 and 200 nM for total Aβ and Aβ42 respectively.- Tzu-Pei Lee, .et al. , Journal of Dental Sciences, 2025, Jul;20(3):1629-1638 PMID: 40654420
- Kubra Telli, .et al. , Turkish Journal of Biochemistry, 2023, February 6
- Paul Mark Medina, .et al. , Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
- Tatsuya Usui, .et al. , Int J Mol Sci, 2018, Apr; 19(4): 1098 PMID: 29642386
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HCV Protease Inhibitor
Boceprevir is a protease inhibitor used as a treatment for hepatitis C genotype 1.- Ueda Y, .et al. , Virus Res, 2017, May 2;235:37-48 PMID: 28322919
- Shirasaki T, .et al. , Hepatology., 2014, 60(5):1519-30 PMID: 24962339
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HCV Protease inhibitor
VX-222 is a small molecule non-nucleoside inhibitor of HCV NS5B polymerase that is being investigated for the treatment of hepatitis C virus infection.- Wataru Ito, .et al. , Antivir Chem Chemother, 2015, Dec; 24(5-6): 148-154 PMID: 27503576
- Hui Shen, .et al. , PLoS One., 2013, 8(12): e82299 PMID: 24358168
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γ-secretase inhibitor
YO-01027 is a dipeptidic γ-secretase inhibitor, an antiAlzheimer agent.- Weijun Zhang, .et al. , Stem Cell Rev Rep, 2023, Jan 7 PMID: 36609902
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Serine/cysteine protease inhibitor
PMSF is an irreversible serine/cysteine protease inhibitor.- Xi Yu, .et al. , Neuroreport, 2022, Nov 2;33(16):705-713 PMID: 36165031
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serine protease inhibitor
Aprotinin is a small protein serine protease inhibitor, used to reduce perioperative blood loss and transfusion.- Xi Yu, .et al. , Neuroreport, 2022, Nov 2;33(16):705-713 PMID: 36165031
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Caspase-1/4 inhibitor
VX-765 is a novel Caspase-1 inhibitor,which is an enzyme that controls the generation of two cytokines, IL-1b and IL-18.- Xianyu Piao, .et al. , Cell Death Differ, 2026, Apr;33(4):717-731 PMID: 41125794
- Takemasa Takii, .et al. , mSphere, 2025, 10:e00110-25 PMID: 40387341
- Joseph Flores, .et al. , Cell Death Dis, 2022, Oct 11;13(10):864 PMID: 36220815
- Arjun Thapa, .et al. , Leukemia, 2021, 23 February PMID: 33623143
- Prenitha Mercy Ignatius Arokia Doss, .et al. , Cell Rep, 2021, Mar 9;34(10):108833 PMID: 33691111
- Joseph Flores, .et al. , Nat Commun, 2020, Sep 11;11(1):4571 PMID: 32917871
- Joseph Flores, .et al. , Nat Commun, 2018, 9: 3916 PMID: 30254377
- Mohamed F. Ali, .et al. , Front Immunol, 2017, 8: 1504 PMID: 29170665
- García-Fernández A, .et al. , J Control Release, 2017, Feb 28;248:60-70 PMID: 28069553
- Jiujiu Yu, .et al. , Proc Natl Acad Sci U S A, 2014, 111(43): 15514-15519 PMID: 25313054
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gamma-secretase modulator
E 2012 is γ-secretase inhibitor.- Yesuvadian R, .et al. , Biochem Biophys Res Commun., 2014, May 16;447(4):590-5 PMID: 24747079
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Gamma-secretase inhibitor
Semagacestat (LY450139) is a γ-secretase blocker for Aβ42, Aβ40 and Aβ38 with IC50 of 10.9 nM, 12.1 nM and 12.0 nM, respectively. Semagacestat also inhibits Notch signaling with IC50 of 14.1 nM.- Yesuvadian R, .et al. , Biochem Biophys Res Commun., 2014, May 16;447(4):590-5 PMID: 24747079
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Apoptosis inducer
LY573636 is a potent anti-tumor agent, which causes growth arrest and apoptosis of a variety of human solid tumors in vitro and in vivo. LY573636-induced apoptosis occurs by a mitochondrial-targeted mechanism.- Yingzheng Xu, .et al. , JCI Insight, 2024, Jun 13:e174746 PMID: 38869957
- Ting TC, .et al. , Cell Rep, 2019, Nov 5;29(6):1499-1510.e6 PMID: 31693891
- Ting Han, .et al. , Science, 2017, Apr 28;356(6336). pii: eaal3755 PMID: 28302793
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Caspase-3 inhibitor
Ivachtin is a potent, cell-permeable, reversible, non-competitive inhibitor of Caspase-3 (IC50 = 23 nM).- Yosefzon Y, .et al. , Mol Cell, 2018, May 17;70(4):573-587.e4 PMID: 29775577
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serine protease inhibitor
Nafamostat is an anticoagulant. Broad spectrum serine protease inhibitor. Reduces eosinophil infiltration, mast cell activation and airway responsiveness in a murine model of asthma.- Zeynep Demirsoy, .et al. , Chemical Engineering Journal, 2025, 516: 164066
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DDP-4 inhibitor
Sitagliptin is an oral antihyperglycemic (anti-diabetic drug) of the dipeptidyl peptidase-4 (DPP-4) inhibitor class.- Zhenhuan Zheng, .et al. , Mol Metab, 2026, Mar 14;106:102340 PMID: 41833222
- Hae Jin Kim, .et al. , Korean J Physiol Pharmacol, 2018, Nov; 22(6): 713-719 PMID: 30402032
- Chintan N. Koyani, .et al. , Front Physiol, 2018, 9: 1622 PMID: 30487758
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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. -
HIV Entry Inhibitor
BMS-806, also known as BMS-378806 , is a type of medicine called an entry inhibitor. Entry inhibitors work by blocking HIV from entering human cells. BMS-378806 (BMS-806) is a small molecule that blocks the binding of host-cell CD4 with viral gp120 protein and therefore inhibits the first steps of HIV-1 infection. -
γ-secretase inhibitor
Begacestat is a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease. -
γ-secretase inhibitor
PF-03084014 is a reversible and selective inhibitor of γ-secretase with IC50 value of 6.2 nM . -
Cathepsin K Inhibitor
Odanacatib is an inhibitor of cathepsin K,an enzyme involved in bone resorption. -
Serine protease inhibitor
BCX 1470 is serine protease inhibitor. BCX 1470 blocks the esterolytic and hemolytic activities of the complement enzymes Cls and factor D in vitro. -
Polymerase inhibitor
Balapiravir (R1626, RG1626) is the prodrug of a nucleoside analogue inhibitor of the hepatitis C virus (HCV) RNA-dependent RNA polymerase (R1479, RG1479). -
γ-Secretase Inhibitor
BMS 433796 is a γ-secretase inhibitor with Aβ lowering activity in a transgenic mouse model of Alzheimer's disease. -
CPA inhibitor
CPA inhibitor is a potent inhibitor for carboxypeptidase A (CPA). -
Gamma-secretase modulator
gamma-secretase modulator 1 is a gamma-secretase modulator, gamma-secretase modulator 1 is useful for Alzheimer's disease. -
Gamma-secretase modulator
gamma-secretase modulator 2 is a potent and selective gamma-secretase modulator for treatment of Alzheimer's disease. -
Cathepsin Inhibitor
Cathepsin Inhibitor 1 is an inhibitor of Cathepsin (L, L2, S, K, B) with pIC50 of 7.9, 6.7, 6.0, 5.5 and 5.2, respectively. -
NAE Inhibitor
NAE inhibitor MLN4924 binds to and inhibits NAE, which may result in the inhibition of tumor cell proliferation and survival. -
NS3 protease inhibitor
Narlaprevir is a potent, selective, orally bioavailable NS3 protease inhibitor(Ki=6 nM; EC90=40 nM)

