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Catalog No.
Product Name
Application
Product Information
Citations
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PPARα/PPARγ Inhibitor
Netoglitazone is a dual agonist targeting PPARα and PPARγ, exhibiting significant antihyperglycemic activity. This compound is instrumental in metabolic research and provides insights into the regulation of glucose homeostasis. Its application in studies related to diabetes and metabolic syndrome makes it a valuable tool for exploring therapeutic strategies. -
PPARγ Inhibitor
trans-Cinnamyl alcohol is a selective PPARγ inhibitor that plays a significant role in regulating lipid metabolism and adipogenesis. As a metabolite derived from chestnut flowers, it exhibits anti-obesity activity by inhibiting PPARγ expression. This compound is valuable for research applications focused on obesity, metabolic disorders, and the modulation of fat cell differentiation. -
mPGES-1/5-LOX Inhibitor
YS121 is a dual inhibitor targeting microsomal prostaglandin E2 synthase-1 (mPGES-1) and 5-lipoxygenase (5-LOX), with IC50 values of 3.4 μM and 6.5 μM, respectively. It demonstrates specific, reversible binding to mPGES-1, indicated by a KD of 10-14 μM. YS121 reduces PGE2 production in IL-1β-stimulated A549 cells with an EC50 of 12 μM and activates PPAR-α and PPAR-γ, with EC50 values of 1 μM and 3.6 μM, respectively. Additionally, YS121 exhibits significant anti-inflammatory effects in human whole blood and in vivo, making it a valuable tool for pleurisy research. -
PPARγ Inhibitor
PPARγ phosphorylation inhibitor 1 is a selective inhibitor targeting Peroxisome Proliferator-Activated Receptor gamma (PPARγ). It effectively inhibits CDK5-mediated phosphorylation of PPARγ at Ser273 with an IC50 of 160 nM, demonstrating a binding affinity with an IC50 of 24 nM. This compound exhibits minimal PPARγ agonistic activity in reporter gene assays, making it a valuable tool for studying the role of PPARγ phosphorylation in metabolic disorders and antidiabetic research applications. -
PPAR-α/δ Inhibitor
Anti-NASH agent 1 is a potent PPAR-α/δ inhibitor that effectively targets nonalcoholic steatohepatitis (NASH). This compound has demonstrated significant efficacy in improving hyperlipidemia, liver fat degeneration, and liver inflammation in a methionine-choline deficiency (MCD) induced NASH mouse model. Additionally, Anti-NASH agent 1 exhibits low liver toxicity while providing protective effects on liver health, making it a valuable tool for research into metabolic disorders and liver diseases. -
PPARγ Inhibitor
Soyasaponin Aa is a PPARγ inhibitor that demonstrates significant anti-obesity effects in 3T3-L1 adipocytes by downregulating the activity of peroxisome proliferator-activated receptor γ. Its biological activity supports research into mechanisms of adipogenesis and metabolic regulation. Soyasaponin Aa is useful in studies aimed at understanding the therapeutic potential of targeting PPARγ in obesity-related conditions. -
Dual ACLY inhibitor/PPARα Agonist
BGT-002 is a potent dual inhibitor of ATP-citrate lyase (ACLY) and a peroxisome proliferator-activated receptor alpha (PPARα) agonist. This compound effectively reduces lipogenesis by inhibiting fatty acid synthesis and enhancing lipid efflux. BGT-002 has shown efficacy in improving metabolic dysfunction-related steatohepatitis and hyperlipidemia in vivo, making it a valuable reagent for research into hypercholesterolemia and related metabolic disorders. -
ATX Inhibitor/PPARγ Agonist
EL244 is a dual inhibitor of Autotaxin (ATX), with an IC50 of 50 nM, and a selective agonist of PPARγ, exhibiting an IC50 of 1.3 μM. This compound shows low cytotoxicity in human HepG2 cells, with an EC50 of 81.2 μM, and minimal inhibition of the cardiac hERG potassium channel (12% at 25 μM). EL244 effectively reduces pulmonary Lysophosphatidic Acid (LPA) levels, mitigates fibrosis, and enhances respiratory function in vivo, making it a valuable tool for the study of idiopathic pulmonary fibrosis and interstitial lung disease (ILD). -
COX-2 Inhibitor/PPAR-γ Activator
Zaltoprofen sulfoxide is a selective COX-2 inhibitor with an IC50 of 45.38 nM, as well as a PPAR-γ activator. This compound effectively inhibits NF-κB and MAPK inflammatory signaling pathways, making it a valuable tool in the study of inflammation and acute lung injury models. It is particularly relevant for research focused on LPS-induced acute lung injury. -
HO-1 Inhibitor
OB-24 is a selective small-molecule inhibitor of heme oxygenase-1 (HO-1), demonstrating an IC50 of 1.9 μM for HO-1 with minimal effect on HO-2 (IC50 > 100 μM). This compound exhibits significant anti-tumor and anti-metastatic activities, making it valuable for research applications in various cancer models, including prostate cancer, melanoma, ovarian carcinoma, and lung metastasis. OB-24 may serve as an essential tool for understanding HO-1's role in tumor progression and metastasis. -
TrxR1 Inhibitor
Aurothioglucose is a potent inhibitor of thioredoxin reductase 1 (TrxR1), exhibiting an IC50 value of 65 nM. This compound effectively inhibits the DNA binding activity of NF-κB in vitro, highlighting its role in modulating key transcriptional pathways. Additionally, Aurothioglucose demonstrates anti-HIV and anti-rheumatic properties, making it a valuable reagent for research in infectious diseases and autoimmune disorders. -
CYP2E1 Inhibitor
CYP2E1-IN-1 is a potent inhibitor of cytochrome P450 2E1 (CYP2E1) with a Kd of 7.02 μM, an IC50 of 1.64 μM, and a Ki of 0.897 μM. This compound activates the Nrf2/HO-1 signaling pathway and effectively inhibits reactive oxygen species (ROS) production, contributing to the alleviation of pancreatic injury. With significant anti-inflammatory and antioxidant properties, CYP2E1-IN-1 is suitable for research applications focused on severe acute pancreatitis and other inflammation-related diseases. -
HO-2 Inhibitor
Heme Oxygenase-2-IN-1 is a selective inhibitor of heme oxygenase-2 (HO-2), demonstrating an IC50 of 0.9 μM for HO-2 and 14.9 μM for HO-1. This compound is valuable in research applications focused on elucidating the role of HO-2 in various biological processes and potential therapeutic interventions. Its specificity for HO-2 makes it a useful tool for studying associated signaling pathways and related diseases. -
Succinate Dehydrogenase Inhibitor
Diethyl butylmalonate is a competitive inhibitor of succinate dehydrogenase, exhibiting anti-inflammatory properties through the reduction of reactive oxygen species (ROS) production. Additionally, it demonstrates neuroprotective effects, making it a valuable tool in studies related to neurodegenerative diseases, including Alzheimer's disease. Furthermore, Diethyl butylmalonate shows toxicity to Tetrahymena pyriformis, with a log(IGC50-1) value of 0.557, underscoring its potential utility in ecological and cellular toxicity research. -
PPO Inhibitor
Trifludimoxazin is a protoporphyrinogen oxidase (PPO) inhibitor with herbicidal properties. By targeting PPO, it leads to the accumulation of reactive oxygen species (ROS) and subsequent cell membrane damage, resulting in effective weed death. Trifludimoxazin demonstrates significant efficacy in managing both broadleaf and grass weeds, making it a valuable tool in agricultural research and weed control applications. -
Lipoxygenase Inhibitor
Aureusidin is a potent lipoxygenase inhibitor known for its significant antioxidant properties. It exhibits anti-inflammatory effects, making it a valuable compound for research focused on inflammatory pathways and oxidative stress responses. Aureusidin is applicable in studies investigating the modulation of lipoxygenase activity and its implications in various diseases. -
Monoamine Oxidase Inhibitor
Nialamide hydrochloride is a non-selective monoamine oxidase (MAO) inhibitor. It effectively inhibits MAO, regulating reactive oxygen species (ROS) production and influencing various physiological responses. This compound induces hyperkinesis in animal models, enhances the anticonvulsant effects of Diphenylhydantoin in mice, and increases rectal temperature while augmenting the pressor response to Norepinephrine. Nialamide hydrochloride is valuable in research focused on depression, inflammatory diseases, neurodegenerative disorders, and hypertension. -
α-Glucosidase Inhibitor
Guavinoside B is an orally active α-glucosidase inhibitor, exhibiting an IC50 of 0.21 mM. It demonstrates significant biological activity by upregulating the expressions of Nrf2, GCLC, and NQO1 while downregulating p-JNK expression and reducing intracellular reactive oxygen species levels. Guavinoside B effectively decreases serum TNF-α levels associated with Acetaminophen, alleviating hepatocellular infiltration and necrosis, and improving liver-related biochemical parameters. This compound is relevant for research in diabetes and Acetaminophen-induced liver injury. -
IDO Inhibitor
Pronqodine A is an inhibitor of Indoleamine 2,3-Dioxygenase (IDO) with an IC50 of 131.5 nM. It effectively reduces bradykinin-induced release of PGE2, 6-keto-prostaglandin F1α, and PGD2, while simultaneously inducing reactive oxygen species (ROS) production in human synovial sarcoma SW982 cells. Additionally, Pronqodine A serves as a substrate for human quinone reductase NQO1, making it a valuable tool for research into inflammation and related biological processes. -
hMAO-B Inhibitor
CHBO4 is a potent, reversible, competitive inhibitor of human monoamine oxidase B (hMAO-B), with an IC50 value of 0.031 μM and a Ki value of 0.010 ± 0.005 μM. This compound demonstrates the ability to reduce cell damage by scavenging intracellular reactive oxygen species (ROS). CHBO4 is suitable for research applications focused on Parkinson's disease (PD) and related neurodegenerative conditions. -
MAO-B Inhibitor
MAO-B-IN-7 is a selective inhibitor of monoamine oxidase B (MAO-B) and acetylcholinesterase (AChE), demonstrating IC50 values of 41 nM for human AChE, 87 nM for electric eel AChE, and 0.3 μM for MAO-B. This compound is notable for its ability to penetrate the blood-brain barrier, making it suitable for central nervous system research. MAO-B-IN-7 has been shown to mitigate oxidative stress and neuroinflammation, supporting its potential applications in neurodegenerative disease studies. -
MAO-B Inhibitor
MAO-B-IN-54 is a selective, reversible, and competitive inhibitor of monoamine oxidase B (MAO-B), exhibiting a human IC50 of 0.052 μM and a Ki of 0.028 μM. This compound demonstrates minimal activity against MAO-A and effectively binds to both the entrance and substrate cavity of MAO-B, establishing hydrophobic and hydrogen bonding interactions. MAO-B-IN-54 has been shown to inhibit amyloid-beta (Aβ) aggregation and reduce reactive oxygen species (ROS) production, making it a valuable tool for research into Alzheimer's disease mechanisms. -
MAO-B Inhibitor
Sembragiline is a potent and selective reversible inhibitor of monoamine oxidase B (MAO-B). By inhibiting MAO-B activity, Sembragiline decreases the metabolism of dopamine and other amine neurotransmitters, potentially increasing their levels within the brain. This inhibition also reduces the formation of toxic reactive oxygen species (ROS), which are implicated in the pathology of Alzheimer's disease (AD). Sembragiline demonstrates favorable oral bioavailability and effective permeability across the blood-brain barrier, making it a valuable tool for research on AD, particularly in patients exhibiting elevated MAO-B activity. -
FAAH Inhibitor
N-Benzyllinolenamide is a natural macamide derived from Lepidium meyenii and acts as an inhibitor of fatty acid amide hydrolase (FAAH) with an IC50 value of 41.8 μM. This compound is valuable for studying the modulation of endocannabinoid signaling pathways and investigating the role of FAAH in various physiological processes. Its ability to inhibit FAAH makes it a useful tool in research related to pain management, inflammation, and neuroprotection. -
HMG-CoA Reductase Inhibitor
(3R,5S)-Fluvastatin sodium is a potent competitive inhibitor of HMG-CoA reductase, displaying an IC50 value of 8 nM. This compound is effective in modulating lipid levels and exhibits protective effects on vascular smooth muscle cells by activating the Nrf2-dependent antioxidant pathway, mitigating oxidative stress. It is widely utilized in cardiovascular research and studies focusing on cholesterol metabolism and oxidative stress responses. -
HMG-CoA Reductase Inhibitor
(3R,5R)-Rosuvastatin is a competitive inhibitor of HMG-CoA reductase, exhibiting an IC50 value of 11 nM. This compound is known for its ability to significantly reduce levels of low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein. Additionally, (3R,5R)-Rosuvastatin has been shown to inhibit human ether-a-go-go related gene (hERG) currents with an IC50 of 195 nM, impacting hERG protein expression and its interactions with heat shock protein 70 (Hsp70). Its pharmacological profile makes it valuable for research related to cholesterol management and cardiovascular health. -
HMG-CoA Reductase Inhibitor
(3S,5R)-Rosuvastatin is a competitive inhibitor of HMG-CoA reductase, exhibiting an IC50 of 11 nM. This agent plays a significant role in reducing low-density lipoprotein (LDL) cholesterol and triglyceride levels while decreasing C-reactive protein levels. Additionally, (3S,5R)-Rosuvastatin inhibits the hERG channel with an IC50 of 195 nM and modulates the expression of the hERG protein through the disruption of its interaction with heat shock protein 70 (Hsp70). This compound is valuable in cardiovascular research and studies focused on cholesterol metabolism. -
HMG-CoA Reductase Inhibitor
(3S,5R)-Fluvastatin-d6 is a deuterium-labeled derivative of the HMG-CoA reductase inhibitor, Fluvastatin. As a competitive inhibitor with an IC50 of 8 nM, it effectively regulates cholesterol biosynthesis. This compound has been shown to protect vascular smooth muscle cells from oxidative stress via the Nrf2-dependent antioxidant pathway, making it a valuable tool in cardiovascular research and studies focused on oxidative damage and cellular stress responses. -
CYP2C9/CYP3A4 Inhibitor
Tetrahydrocurcumin-d6 is a deuterated analog of Tetrahydrocurcumin, functioning as an inhibitor of CYP2C9 and CYP3A4 enzymes. This compound exhibits significant biological activity against these cytochrome P450 isoforms, making it valuable for research into drug metabolism and pharmacokinetics. Tetrahydrocurcumin-d6 is utilized in studies aiming to elucidate the metabolic pathways and interactions of curcuminoids, as well as their potential therapeutic applications. -
HMG-CoA Reductase Inhibitor
Atorvastatin strontium is an HMG-CoA reductase inhibitor that effectively lowers cholesterol levels, impacting cardiovascular health. Its primary mechanism involves the inhibition of HMG-CoA reductase in liver tissue, which plays a crucial role in cholesterol synthesis. This compound is also utilized in research to address dyslipidemia and related metabolic disorders. -
FAAH Inhibitor
SA72 is a highly selective inhibitor of fatty acid amide hydrolase (FAAH), an enzyme crucial for the degradation of endocannabinoids. By inhibiting FAAH, SA72 modulates endocannabinoid levels, leading to potential therapeutic effects in pain management and inflammation. This compound serves as a valuable tool in research aimed at understanding the endocannabinoid system and its role in various physiological processes. -
Cathepsin G Inhibitor
Cathepsin G Inhibitor I is a potent and selective reversible competitive inhibitor of Cathepsin G, exhibiting an IC50 value of 53 nM and a Ki of 63 nM. This non-peptidic compound is primarily utilized in research investigating immune disorders, providing valuable insights into the role of Cathepsin G in various pathogenic processes. Its specificity makes it a useful tool for understanding the implications of Cathepsin G in immune system regulation. -
Cathepsin L Inhibitor
Cathepsin L-IN-2 is a selective inhibitor of Cathepsin L, exhibiting an IC50 of 15 μM. This compound irreversibly inhibits the proteolytic activity of cathepsins by covalently binding to cysteine residues in the enzyme's active site. Cathepsin L-IN-2 is primarily utilized in research focused on neurodegenerative diseases, including GRN-related frontotemporal dementia, as well as in studies investigating cancer invasion and metastasis. -
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. -
Cathepsin X Inhibitor
Cathepsin X-IN-1 is a potent inhibitor of Cathepsin X, exhibiting an IC50 of 7.13 µM. This compound effectively reduces PC-3 cell migration while demonstrating low cytotoxicity. It serves as a valuable tool in cancer research, particularly in studies focused on metastatic processes and the modulation of proteolytic enzymes. -
Cysteine Cathepsin Inhibitor
JPM-OEt is a potent cysteine cathepsin inhibitor that binds covalently to the active site, irreversibly inhibiting the cysteine cathepsin family. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its ability to modulate cysteine cathepsins expands its potential applications in studying various pathophysiological processes and therapeutic interventions. -
Cathepsin Inhibitor
Aurantiamide acetate is a selective and orally active inhibitor of cathepsins, derived from the plant Portulaca oleracea L. This compound exhibits significant anti-inflammatory properties, making it valuable for investigating the mechanisms underlying inflammatory diseases. Researchers can utilize aurantiamide acetate to explore therapeutic strategies aimed at modulating cathepsin activity in various pathological conditions. -
Cathepsin L Inhibitor
KGP94 is a selective inhibitor of cathepsin L, exhibiting an IC50 value of 189 nM. This compound effectively inhibits the migration and invasion of metastatic carcinoma while demonstrating low cytotoxicity with a GI50 of 26.9 µM across various human cell lines. KGP94 is suitable for research applications focused on cancer biology and the modulation of proteolytic enzyme activity. -
Cathepsin-L Inhibitor
Z-FF-FMK is a selective inhibitor of cathepsin L, primarily known for its role in regulating apoptotic processes. This compound effectively prevents β-amyloid-induced apoptotic changes, including the activation of caspase-3, cleavage of poly-ADP ribose polymerase, and subsequent DNA fragmentation. Z-FF-FMK is valuable in research applications focused on neurodegenerative diseases and the role of proteolytic enzymes in apoptosis. -
Cathepsins Inhibitor
Relacatib is a potent, orally active inhibitor of human cathepsins K, L, and V, demonstrating Ki values of 41 pM, 68 pM, and 53 pM, respectively. This compound effectively inhibits endogenous cathepsin K in situ within human osteoclasts, significantly impacting osteoclast-mediated bone resorption with IC50 values of 45 nM and 70 nM. Relacatib shows promise in preclinical research for reducing bone resorption both in vitro using human tissue and in vivo studies in cynomolgus monkeys. -
Cathepsin C Inhibitor
Cathepsin C-IN-5 is a selective inhibitor of Cathepsin C, exhibiting an IC50 of 59.9 nM, with minimal activity against other cathepsins such as Cat L (4.26 µM) and others (>5 µM). This compound effectively inhibits Cathepsin C activity in bone marrow and blood, leading to a reduction in the activation of neutrophil serine proteases (NSPs). Its anti-inflammatory properties make Cathepsin C-IN-5 a valuable tool for research exploring inflammatory disorders and related pathways. -
Cathepsin D Inhibitor
CatD-IN-1 is a selective inhibitor of cathepsin D, demonstrating an IC50 of 0.44 μM. This compound serves as a valuable tool for investigating the biochemical pathways involved in osteoarthritis research. Its specific inhibition of cathepsin D may facilitate studies on tissue remodeling and degeneration associated with joint diseases. -
AEP Inhibitor
AEP-IN-2 is an inhibitor of asparagine endopeptidase (AEP), effectively blocking the cleavage of amyloid precursor protein (APP) and tau protein. This compound exhibits oral bioactivity and is capable of reducing levels of amyloid beta 40 (Aβ40), amyloid beta 42 (Aβ42), and phosphorylated tau (p-Tau). AEP-IN-2 is utilized in research applications focused on neurodegenerative diseases and the modulation of protein aggregation pathways. -
Cathepsin Inhibitor
Cathepsin Inhibitor 2 is a highly potent inhibitor of Cathepsin S, exhibiting a Ki value of less than 20 nM. This compound is primarily utilized in research to investigate the role of cathepsins in various biological processes, including protein degradation and immune responses. It serves as a valuable tool for studies related to cancer, inflammation, and other conditions where Cathepsin S activity is a contributing factor. -
Cathepsin K Inhibitor
ONO-5334 is a potent and selective inhibitor of cathepsin K, exhibiting Ki values of 0.10 nM, 0.049 nM, and 0.85 nM for human, rabbit, and rat cathepsin K, respectively. This compound also demonstrates significant antiviral activity against SARS-CoV-2, with an EC50 value of 500 nM. ONO-5334 is valuable for research applications involving osteoporosis and COVID-19, facilitating the exploration of therapeutic interventions targeting these conditions. -
Cysteine Protease Cathepsin K Inhibitor
2-Cyanopyrimidine is a potent inhibitor of cysteine protease cathepsin K, exhibiting an IC50 value of 170 nM. This compound demonstrates significant biological activity in the modulation of bone resorption and is being investigated for its potential therapeutic applications in osteoporosis. Researchers can utilize 2-Cyanopyrimidine to study the role of cathepsin K in bone metabolism and related disorders. -
Cathepsin L Inhibitor
3-Epiursolic Acid is a triterpenoid compound that functions as a competitive inhibitor of cathepsin L, demonstrating an IC50 value of 6.5 μM and a Ki value of 19.5 μM. This compound exhibits selectivity for cathepsin L without significantly affecting cathepsin B. Its inhibitory properties make it valuable for research into protease inhibition and related biological pathways. -
Cathepsin L Inhibitor
Z-Phe-Tyr(tBu)-diazomethylketone is a potent inhibitor of cathepsin L, an enzyme involved in various cellular processes. This compound has been shown to facilitate the disassembly of reovirus, thereby reducing viral detection levels. It serves as a valuable tool in research applications targeting viral infections and evaluating the role of cathepsin L in disease mechanisms. -
Cathepsins Inhibitor
Z-DEVD-CMK is an irreversible inhibitor targeting cathepsins, demonstrating potent activity against various cathepsin isoforms in vitro. This compound is utilized in research to study the role of cathepsins in apoptosis, inflammation, and cancer progression. It serves as a valuable tool for elucidating the functional mechanisms of cathepsins in biological systems. -
Cathepsin G/Chymase Inhibitor
JNJ-10311795 is a potent dual inhibitor targeting neutrophil cathepsin G (Ki = 38 nM) and mast cell chymase (Ki = 2.3 nM). This compound demonstrates significant anti-inflammatory properties, making it valuable for research aimed at elucidating the roles of these proteases in inflammatory diseases. Its specificity and efficacy render it suitable for studies focused on developing therapeutics for conditions associated with excessive inflammation.
