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Catalog No.
Product Name
Application
Product Information
Citations
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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 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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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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DPP4 Inhibitor
Evogliptin is an orally active inhibitor of DPP4 (dipeptidyl peptidase-4), demonstrating notable and sustained hypoglycemic effects in murine models. In addition to its antidiabetic properties, Evogliptin exerts effects by inhibiting the production of inflammatory and fibrotic signals in hepatocytes through the induction of autophagy. This compound is particularly relevant for research applications related to type 2 diabetes, osteoporosis, renal impairment, and chronic liver inflammation. -
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. -
DPP4 Inhibitor
(Rac)-Sitagliptin is a potent and selective inhibitor of dipeptidyl peptidase-4 (DPP4), exhibiting an IC50 of 19 nM in Caco-2 cell extracts. This compound plays a significant role in the modulation of glucose metabolism, making it relevant for diabetes research. Its ability to enhance insulin secretion and decrease glucagon levels underscores its potential applications in studying metabolic disorders and developing therapeutic strategies for type 2 diabetes. -
Calpain/Cathepsin Inhibitor
ALLM, also known as Calpain inhibitor II, acts as a potent inhibitor of calpain and cathepsin proteases. This compound is known to mitigate neuronal cell death, thereby enhancing chronic neurological function following spinal cord injury (SCI). Its utility in research extends to studies investigating protease activity and the mechanisms underlying neuroprotection in trauma-related conditions. -
Calpain Inhibitor
(Rac)-Neurodegenerative Disorder-Targeting Compound 1 is a calpain inhibitor that selectively modulates calpain activity, implicated in neurodegenerative processes. This compound is designed for research applications focused on neurodegeneration, providing a valuable tool for investigating the role of calpain in cellular function and injury. The inhibition of calpain activity may contribute to understanding the molecular mechanisms underlying neurodegenerative disorders. -
Tyrosinase Inhibitor
Swertiajaponin is a potent tyrosinase inhibitor that interacts with the enzyme's binding pocket through hydrogen bonding and hydrophobic interactions, exhibiting an IC50 of 43.47 μM. It effectively inhibits oxidative stress-mediated MAPK/MITF signaling pathways, resulting in a reduction of tyrosinase protein levels. Additionally, Swertiajaponin demonstrates strong anti-oxidative activity and suppresses melanin accumulation, making it a valuable tool for research aimed at understanding pigmentation disorders and oxidative stress. -
Aldose reductase Inhibitor
Danshenol A is a potent aldose reductase inhibitor, exhibiting an IC50 of 0.1 μM. This abietane-type diterpenoid demonstrates protective effects on endothelial cells against oxidative stress through direct scavenging of reactive oxygen species (ROS). Additionally, Danshenol A possesses notable anti-inflammatory and antitumor properties, making it a valuable compound for research focused on atherosclerosis and related pathologies. -
DPP-4 Inhibitor
PB01 is a selective DPP-4 inhibitor with an IC50 of 15.66 nM. It effectively reduces high glucose-induced reactive oxygen species (ROS) production and mitochondrial superoxide generation while significantly decreasing cellular DPP-4 expression. In vivo studies demonstrate that PB01 can lower blood glucose levels in diabetic mice, indicating its potential therapeutic application. Furthermore, PB01 exhibits minimal cytotoxicity at a concentration of 100 μM, making it a promising candidate for diabetes-related research. -
Tyrosinase Inhibitor
Tyrosinase-IN-12 is a potent non-competitive inhibitor of tyrosinase, demonstrating an IC50 value of 49.33 ± 2.64 µM and a Ki value of 31.25 ± 0.25 µM. This compound exhibits strong radical scavenging activity, effectively reducing the production of reactive oxygen species (ROS) with an IC50 of 25.39 ± 0.77 µM. Tyrosinase-IN-12 is applicable in research focusing on the mitigation of browning in food products and agricultural applications. -
DPP-IV Inhibitor
DPP-4-IN-3 is a potent inhibitor of dipeptidyl peptidase IV (DPP-IV), exhibiting an IC50 value of 0.75 nM. This compound demonstrates significant antioxidant properties alongside insulinotropic activity, making it a valuable tool for diabetes research and the study of metabolic disorders. Its ability to modulate the DPP-IV pathway underscores its potential in therapeutic applications aimed at enhancing glucose homeostasis. -
cACE/NEP Inhibitor
AD012 is a dual inhibitor of the enzymes neprilysin (NEP) and angiotensin-converting enzyme (cACE). Designed from the C-domain selective ACE inhibitor, lisinopril-tryptophan, AD012 demonstrates significant antihypertensive and cardioprotective properties. This compound is valuable for research in cardiovascular health and the treatment of hypertension. -
NEP Inhibitor
GW 796406 is a potent neprilysin (NEP) inhibitor with an IC50 value of approximately 1.1-2.5 nM, exhibiting a higher selectivity compared to ACE, which has an IC50 of around 1.6-4.7 nM. This compound is valuable for exploring mechanisms involved in cardiovascular diseases and may aid in the development of therapeutics targeting NEP-related pathways. GW 796406's specificity and efficacy make it a useful tool for researchers studying cardiovascular health and related disorders. -
ACE/NEP Inhibitor
RB-105 is a potent dual inhibitor of angiotensin-converting enzyme (ACE) and neutral endopeptidase (NEP), with Ki values of 4.2 nM and 1.7 nM, respectively. By inhibiting ACE, RB-105 decreases angiotensin II production and enhances bradykinin levels, while NEP inhibition further elevates natriuretic peptide levels, resulting in a synergistic increase in bradykinin. This compound exhibits significant antihypertensive and natriuretic effects in both spontaneously hypertensive and normotensive rat models, making RB-105 a valuable reagent for studies on hypertension and related cardiovascular conditions. -
NEP/ACE Inhibitor
Aladotril, a dual inhibitor of neutral endopeptidase (NEP) and angiotensin-converting enzyme (ACE), exhibits potential in ameliorating cardiac hypertrophy without reducing blood pressure. This compound is valuable for research focused on heart failure and the mechanisms of cardiac remodeling following myocardial infarction. Its unique properties make it an important tool for studying cardiovascular health and therapeutic interventions. -
ACE/ECE-1/NEP Inhibitor
CGS 35601 is a potent inhibitor of endothelin-converting enzyme-1 (ECE-1), neutral endopeptidase 24.11 (NEP), and angiotensin-converting enzyme (ACE), exhibiting IC50 values of 55 nM, 2 nM, and 22 nM, respectively. This compound effectively suppresses pressor responses induced by big endothelin-1 and angiotensin I, while simultaneously enhancing the circulation of atrial natriuretic peptide (ANP). CGS 35601 serves as a valuable tool in cardiovascular research, particularly in delineating the regulatory mechanisms of cardiovascular function in animal models. -
Angiotensin-Converting Enzyme/Neprilysin Inhibitor
Alatrioprilat is an orally active inhibitor of angiotensin-converting enzyme (ACE) and neprilysin, with an IC50 of 19.6 nM for ACE and 6.1 nM for neprilysin. This compound is significant in the metabolism of hormonal peptides, particularly in the degradation of nitric oxide and atrial natriuretic factor (ANF). Alatrioprilat is applicable in cardiovascular disease research, offering insights into therapeutic strategies for conditions influenced by these pathways. -
Glutamine Synthetase Inhibitor
JFD01307SC is a selective inhibitor of glutamine synthetase, which plays a crucial role in the conversion of L-glutamate to glutamine. By mimicking L-glutamate, JFD01307SC effectively targets and modulates the enzymes involved in glutamine biosynthesis. This compound is primarily utilized in research related to tuberculosis and other metabolic disorders, providing valuable insights into the therapeutic potential of glutamine metabolism modulation. -
DPP4 Inhibitor
Evogliptin tartrate is an orally active DPP4 inhibitor that exhibits significant and sustained hypoglycemic effects in murine models. It not only lowers blood glucose levels but also attenuates the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. This compound is suitable for research applications related to type 2 diabetes, osteoporosis, renal impairment, and chronic liver inflammation. -
DHODH Inhibitor
DHODH-IN-8 is a selective inhibitor of dihydroorotate dehydrogenase (DHODH) in both human and Plasmodium falciparum, exhibiting IC50 values of 0.13 μM and 47.4 μM, respectively. Additionally, it demonstrates Kis of 0.016 μM for human DHODH and 5.6 μM for the parasite's enzyme. This compound shows significant antimalarial activity, making it a valuable tool for research into malaria treatment and the inhibition of the pyrimidine biosynthesis pathway. -
DHODH Inhibitor
DHODH-IN-20 is a potent inhibitor of dihydroorotate dehydrogenase (DHODH), an iron-containing flavin-dependent enzyme located in the inner mitochondrial membrane of human cells. By inhibiting DHODH, this compound exhibits significant anti-tumor activity, making it a valuable tool in the study of cancer biology. DHODH-IN-20 is particularly relevant for research focused on acute myelogenous leukemia, offering insights into potential therapeutic strategies. -
HsDHODH Inhibitor
DHODH-IN-3 is a selective inhibitor of Human Dihydroorotate Dehydrogenase (HsDHODH), demonstrating a potent inhibitory effect with an IC50 value of 261 nM. By targeting the ubiquinone binding sites within the enzyme, DHODH-IN-3 exhibits a competitive inhibition profile, characterized by a Kiapp of 32 nM. This compound shows promise for therapeutic applications in malaria research, potentially contributing to the development of novel treatments. -
DHODH Inhibitor
DHODH-IN-12 is a derivative of Leflunomide that functions as a dihydroorotate dehydrogenase (DHODH) inhibitor. This compound displays weak inhibitory activity against DHODH, making it a valuable tool for studying the modulation of pyrimidine metabolism. Its applications include investigations into immunological diseases and the development of therapeutics targeting nucleotide synthesis pathways. The pKa of 5.07 further informs its solubility and stability characteristics in biological systems. -
hDHODH Inhibitor
hDHODH-IN-2 is a selective inhibitor of human dihydroorotate dehydrogenase (hDHODH), functioning as an analogue of Leflunomide's active metabolite. This compound exhibits anti-inflammatory properties, making it relevant for research into autoimmune diseases and other inflammatory conditions. Its mechanism of action targets pyrimidine synthesis, effectively reducing the production of lymphocytes involved in inflammatory responses. -
DHODH Inhibitor
DHODH-IN-13 is a potent inhibitor of dihydroorotate dehydrogenase (DHODH), displaying an IC50 of 4.3 μM for rat liver DHODH. This hydroxyfurazan analog of A771726 demonstrates significant biological activity in modulating pyrimidine metabolism. DHODH-IN-13 is primarily utilized in research related to rheumatoid arthritis and other autoimmune conditions, making it a valuable tool for exploring therapeutic strategies in these areas. -
hDHODH Inhibitor
hDHODH-IN-14 is a potent inhibitor of human dihydroorotate dehydrogenase (hDHODH), exhibiting an IC50 value of 0.469 μM. This compound is utilized primarily in research focused on modulating the de novo pyrimidine biosynthesis pathway. Its inhibitory effects make hDHODH-IN-14 a valuable reagent for studying metabolic processes and potential therapeutic strategies in various diseases, including autoimmune disorders and cancer. -
DHODH Inhibitor
DHODH-IN-19 is a potent inhibitor of dihydroorotate dehydrogenase (DHODH), an essential enzyme located in the inner membrane of human mitochondria that is critical for pyrimidine biosynthesis. This compound demonstrates significant anticancer activity by inhibiting tumor growth, making it a valuable tool for research in cancer and inflammatory diseases. Its mechanism of action offers potential insights into the metabolic pathways involved in these conditions. -
DHODH Inhibitor
hDHODH-IN-7 is a selective inhibitor of human dihydroorotate dehydrogenase (DHODH). It exhibits antiviral activity with a reported pMIC50 of 7.4, indicating its potential efficacy in reducing viral replication. This compound is suitable for research applications involving the study of viral infections and the regulation of pyrimidine biosynthesis. -
DHODH Inhibitor
DHODH-IN-15 is a potent dihydroorotate dehydrogenase (DHODH) inhibitor, exhibiting an IC50 of 11 μM in rat liver DHODH assays. This hydroxyfurazan analog of A771726 demonstrates significant biological activity, making it a valuable tool for investigating the role of DHODH in various metabolic pathways. Its application extends to research on rheumatoid arthritis, contributing to the understanding of therapeutic strategies for inflammatory diseases.
