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Catalog No.
Product Name
Application
Product Information
Product Citation
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HIV Protease Inhibitor
Saquinavir mesylate is an HIV Protease Inhibitor used in antiretroviral therapy. -
HCV NS3/4A protease inhibitor
Simeprevir is a potent inhibitor of HCV NS3/4A protease (Ki = 0.36 nM) and viral replication (replicon EC50 = 7.8 nM). - Camostat mesylate is an orally active protease inhibitor. Known to inhibit trypsin and various inflammatory proteases including plasmin, kallikrein and thrombin.
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Thrombin inhibitor
Argatroban is an anticoagulant that is a small molecule direct thrombin inhibitor. -
Aldose reductase inhibitor
Fidarestat (SNK 860) is an inhibitor of aldose reductase, with IC50s of 26 nM, 33 μM, and 1.8 μM for aldose reductase, AKR1B10 and V301L AKR1B10, respectively; Fidarestat (SNK 860) has the potential to treat diabetic disease. -
PP2A inhibitor
Calyculin A is a potent and cell-permeable protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A) inhibitor with IC50s of 2 nM and 0.5-1 nM. -
HIV protease inhibitor
Darunavir Ethanolate (Prezista) is an HIV protease inhibitor. - Indinavir sulfate is a novel hydroxyaminopentane amide class of HIV-1 protease inhibitors.
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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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Apoptosis Activator
Apoptosis Activator 2 strongly induces caspase-3 activation, PARP cleavage, and DNA fragmentation which leads to the destruction of cells (Apaf-1 dependent) with IC50 of ~4 μM, inactive to HMEC, PREC, or MCF-10A cells - 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
- Arctigenin is an antioxidant, anti-inflammatory, antiproliferative and antiviral agent. It inhibits LPS-induced iNOS expression via inhibition of IκBα phosphorylation and p65 nuclear translocation (IC50 = 10 nM)
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p32-kinase activator
D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator. -
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.- 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
- Hannes Schmid, .et al. , Haematologica, 2021, Jan 14 PMID: 33440919
- 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
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Thrombin inhibitor
Ximelagatran is an anticoagulant that has been investigated extensively as a replacement for warfarin that would overcome the problematic dietary, drug interaction, and monitoring issues associated with warfarin therapy. -
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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Caspase-6 inhibitor
Z-VEID-FMK is the specific recognition sequence for caspase-6/Mch2. Z-VEID-FMK is a synthetic peptide that irreversibly inhibits activity of VEID-dependent caspases (e.g., caspase-6). The inhibitor is designed as a methyl ester to facilitate cell permeability. -
Caspase-2 inhibitor
Z-VDVAD-FMK is a cell-permeable, irreversible inhibitor of caspase-2. Caspase inhibitors play an important role in investigating biological processes. -
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.- 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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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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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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neutrophil elastase inhibitor
Avelestat, also known as AZD9668, is a novel, oral inhibitor of neutrophil elastase (NE). -
SHIP1 Inhibitor
3AC is a cell-permeable, selective inhibitor of SHIP1 polyphosphatase activity toward PIP3 (IC50 = 10 μM), but has no effect on SHIP2 or PTEN activity on PIP3. -
MMP inhibitor
Marimastat acted as a broad-spectrum matrix metalloproteinase inhibitor.- 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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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. - Prodipine, a diphenyl-phosphonate derivative. The IC50s of Prodipine for purified and plasma Dipeptidyl peptidase IV (DPP IV) from the rabbit are 4.5 μM and 30 μM, respectively.
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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.- 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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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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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
- Trifloxystrobin (CGA 279202) is a fungicide, with EC50s of 23.0 μg/L and 1.7 μg/L for Daphnia magna neonate and embryos, respectively, after treatment for 48 h.
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HIV-1 RT inhibitor
Trovirdine inhibits HIV-1 RT with an IC50 of 7 nM when employing heteropolymeric primer/template (oligo-DNA/ribosomal RNA)and dGTP as substrate. -
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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Cysteine Protease inhibitor
Loxistatin Acid, a derivative of E-64, is an irreversible and membrane-permeant cysteine protease inhibitor. -
Cysteine Protease inhibitor
E-64d is an inhibitor of cathepsins B and L and it is lysosome and cell permeable.- 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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DPP-4 inhibitor
Omarigliptin (MK-3102) is a competitive, reversible inhibitor of DPP-4 (IC50 = 1.6 nM, Ki = 0.8 nM). It is highly selective over all proteases tested (IC50 > 67 μM), including QPP, FAP, PEP, DPP8, and DPP9 and has weak ion channel activity (IC50 > 30 μM at IKr, Caγ1.2, and Naγ1.5). -
DPP-4 inhibitor
Alogliptin Benzoate is a dipeptidyl-peptidase-4 (DPP 4) inhibitor -
DPP-4 inhibitor
Trelagliptin is a long acting dipeptidyl peptidase-4 (DPP-4) inhibitor that is being developed for the treatment of type 2 diabetes (T2D). -
dual TACE/MMPs inhibitor
Apratastat is an orally active, potent, and reversible dual inhibitor of tumor necrosis factor-α converting enzyme (TACE) and matrix metalloproteinases (MMPs) . - FABP4 Inhibitor is a cell-permeable biphenylazolo-oxyacetate that acts as a potent and selective inhibitor of adipocyte Fatty-Acid-Binding Protein (aFABP/aP2) by targeting its fatty acid-binding pocket (Ki = < 2 nM in a competitive binding assay using 1,8-ANS), while exhibiting much lower affinity for muscle and epidermal FABP's (Ki = 250 nM and 350 nM, respectively).
- 4-Butylresorcinol is a phenol derivative which can inhibit tyrosinase with IC50 of 11.27 μM.
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Caspase-3 Inhibitor
Z-DEVD-FMK is a specific, irreversible Caspase-3 inhibitor.- 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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DPP-4 inhibitor
Alogliptin is a potent, selective inhibitor of DPP-4 with IC50 of <10 nM, exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9.