Catalog No.
Product Name
Application
Product Information
Citations
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Cathepsin B Substrate
Z-Arg-Arg-AMC is a selective substrate for cathepsin B, a cysteine protease involved in various physiological and pathological processes. This compound facilitates the measurement of cathepsin B activity through the release of a freely diffusible fluorophore. It is commonly utilized in biochemical assays to study protease activity, including research on cancer, inflammation, and other diseases associated with altered cathepsin levels. -
Cathepsin K inhibitor
Cathepsin K inhibitor 5 is a selective inhibitor of Cathepsin K, a cysteine protease involved in bone resorption and remodeling. This compound effectively inhibits Cathepsin K activity, making it valuable for studying osteoclast function and bone-related diseases such as osteoporosis. Its use in research can enhance understanding of bone metabolism and aid in the development of novel therapeutic strategies for bone disorders. -
Cathepsin D inhibitor
TB-9 is a potent inhibitor of cathepsin D, cathepsin E, and BACE1, exhibiting IC50 values of 0.0783 nM, 0.724 nM, and 54.2 nM, respectively. This compound shows significant potential in the study of neurodegenerative diseases and cancer, where cathepsin activity is implicated. Its ability to selectively target these enzymes makes TB-9 an important tool for researchers investigating the role of proteases in various biological processes. -
Cathepsin K Inhibitor
Cathepsin K-IN-8 is a potent inhibitor of cathepsin K, an enzyme involved in the degradation of extracellular matrix components. This compound is primarily utilized in research focused on inflammatory diseases such as rheumatoid arthritis and osteoarthritis, as well as conditions like osteoporosis and tumor progression. Its inhibition of cathepsin K allows for the investigation of its role in these pathological processes, making it a valuable tool for studying bone resorption and related disorders. -
peptides
Cathepsin E substrate e is a selective substrate for the enzyme Cathepsin E, designed to facilitate monitoring of its proteolytic activity. This substrate employs a close proximity of a Mca donor and a Dnp acceptor to create a near-complete intramolecular quenching effect in its intact form. Upon cleavage by Cathepsin E, the spatial separation of Mca and Dnp generates a significant increase in fluorescence, making it an effective tool for studying Cathepsin E activity and its role in various biological processes. -
Cathepsin S Inhibitor
BI-1124 is a selective inhibitor of cathepsin S, a cysteine protease involved in various pathological processes, including inflammation and tissue remodeling. This compound demonstrates effective ocular pharmacokinetic-pharmacodynamic properties in rabbit models following topical administration. BI-1124 is primarily utilized in research focused on age-related dry eye disease, making it a valuable tool for exploring therapeutic interventions in ocular health. -
Cathepsin Inhibitor
Z-FG-NHO-Bz is a selective inhibitor of cathepsins, a family of cysteine proteases involved in various biological processes. This compound exhibits significant inhibitory activity against cathepsin B and L, making it a valuable tool for studying their roles in pathological conditions such as cancer and neurodegenerative diseases. Z-FG-NHO-Bz is ideal for research applications focused on proteolytic enzyme regulation and therapeutic intervention. -
Cathepsin K Inhibitor
Dutacatib is a selective inhibitor of cathepsin K with demonstrated antiviral activity against SARS-CoV-2 3CLpro. By inhibiting cathepsin K, it plays a role in ameliorating bone diseases associated with cancer. This compound is valuable for research focused on therapeutic interventions in viral infections and bone-related pathologies in cancer. -
Cathepsin B Substrate
S2160 is a specific substrate for Cathepsin B, designed for use in calorimetric assays. This compound enables the accurate measurement of Cathepsin B activity in various biological samples. Researchers can utilize S2160 to study proteolytic processes and explore the role of Cathepsin B in physiological and pathological conditions. -
Cathepsin E Inhibitor
SQ 32602 is a potent inhibitor of cathepsin E, exhibiting an IC50 value of 88 nM. This compound selectively inhibits cathepsin E activity, making it valuable for research into lysosomal function and proteolytic processes. SQ 32602 is suitable for studies involving cancer biology, autoimmune diseases, and other conditions where cathepsin E modulation may play a critical role. -
Cathepsin Inhibitor
NC 2300 is a selective and orally active inhibitor of cysteine cathepsins, specifically targeting cathepsin B, K, and S with IC50 values of 284, 34.5, and 186 nM, respectively. This compound is particularly useful in the study of diseases related to bone mineral disorders, enabling researchers to explore the role of cathepsins in these conditions and potential therapeutic interventions. -
Cathepsin D Inhibitor
TB-11 is a potent Cathepsin D inhibitor, demonstrating an IC50 of 0.126 nM for Cathepsin D, alongside inhibitory activity of 1.92 nM for Cathepsin E and 48.8 nM for BACE1. This compound is valuable for research focused on tumor biology and the role of cathepsins in cancer progression. Its selectivity and potency make it a useful tool for investigating the therapeutic potential of Cathepsin D inhibition in various oncological studies. -
Cathepsin K Inhibitor
Cathepsin K-IN-9 is a potent and selective inhibitor of Cathepsin K, exhibiting an IC50 of 6.2 nM. It demonstrates remarkable selectivity with IC50 values exceeding 10,000 nM for Cathepsins B, L, and S, providing over 1600-fold selectivity. With its excellent safety profile and metabolic stability, Cathepsin K-IN-9 is suitable for research applications in osteoporosis and other bone resorption-related studies. -
MPro/Cathepsin L Inhibitor
MPI8 is an inhibitor of the major protease of SARS-CoV-2 (MPro) and cathepsin L, exhibiting significant antiviral activity. It functions through dual and selective inhibition of these key proteases, impacting the viral life cycle and host cellular processes. MPI8 is suitable for use in clinical studies targeting COVID-19 and contributes to understanding therapeutic strategies against SARS-CoV-2. -
cathepsin K Inhibitor
BML-244 is a potent inhibitor of cathepsin K, a cysteine proteinase involved in various pathological processes. This compound demonstrates significant biological activity in the context of inflammatory conditions, making it valuable for research applications related to rheumatoid arthritis (RA) and periodontitis. The inhibition of cathepsin K by BML-244 facilitates the exploration of its role in bone resorption and tissue remodeling, contributing to a better understanding of these diseases. -
Cathepsin S Inhibitor
Cathepsin S-IN-1 is a potent inhibitor of Cathepsin S, a cysteine protease involved in the regulation of immune responses and antigen processing. By selectively targeting Cathepsin S, this compound can modulate inflammatory pathways and contribute to studies on autoimmune diseases, cancer, and other pathological conditions linked to protease activity. Its application in research may provide insights into therapeutic strategies aimed at inhibiting Cathepsin S-mediated processes. -
Neutrophil Cathepsin G Inhibitor
MDL 27399 is a selective inhibitor of human neutrophil cathepsin G, exhibiting a Ki value of 7 μM. This compound is instrumental in studying the role of cathepsin G in inflammatory diseases, allowing researchers to explore potential therapeutic avenues for conditions characterized by excessive neutrophil activity. -
CYP2C8 Inhibitor
Gemfibrozil 1-O-β-glucuronide is a competitive inhibitor of the CYP2C8 enzyme, exhibiting an IC50 of 4.07 μM. As a metabolite of Gemfibrozil, this compound plays a significant role in studying drug metabolism and interactions, particularly within the context of lipid metabolism and therapeutic drug monitoring. Its inhibition capacity makes it relevant for research focused on pharmacokinetics and the effects of CYP2C8 modulation on drug efficacy and safety. -
Pan-PPAR Agonist, HIF-1α Inhibitor
Bavachinin is a pan-peroxisome proliferator-activated receptor (PPAR) agonist and a HIF-1α inhibitor, demonstrating IC50 values of 21.043 μM, 12.819 μM, and 0.622 μM for PPAR-α, PPAR-β/δ, and PPAR-γ, respectively. This compound exhibits significant antitumor activity against non-small cell lung cancer through its modulation of PPAR-γ. Additionally, Bavachinin possesses notable anti-inflammatory and anti-angiogenic properties, making it a valuable tool for research in cancer and metabolic disorders. Its oral bioavailability further supports its utility in various biological studies. -
PPARG Inverse Agonist
FX-909 is a covalent inverse agonist of peroxisome proliferator-activated receptor gamma (PPARG), functioning through modulation of receptor activity. This compound exhibits promising biological activity by inhibiting PPARG-mediated signaling pathways, which are often implicated in cancer progression. FX-909 is utilized in cancer research to investigate the effects of PPARG inhibition on tumor growth and survival, providing insights into potential therapeutic targets. -
PPARγ/PPARδ Agonist
15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is an endogenous cyclopentenone prostaglandin that targets peroxisome proliferator-activated receptors, specifically acting as a selective agonist for PPARγ with an EC50 of 2 µM and a covalent agonist for PPARδ. This compound is known to facilitate the differentiation of C3H10T1/2 fibroblasts into adipocytes with an EC50 of 7 μM. Due to its effects on adipogenesis and metabolism, 15d-PGJ2 is utilized in research exploring obesity, diabetes, and metabolic syndrome pathways. -
PPARδ Agonist
Seladelpar sodium salt is a potent and selective agonist of the PPARδ receptor, demonstrating an EC50 of 2 nM. It exhibits more than 750-fold selectivity over PPARα and 2500-fold selectivity over PPARγ. This compound is primarily utilized in research regarding primary biliary cholangitis, contributing to the understanding of metabolic and inflammatory pathways. -
PPARγ Antagonist
SR1664 is a potent antagonist of peroxisome proliferator-activated receptor gamma (PPARγ). It effectively binds to PPARγ and inhibits Cdk5-mediated phosphorylation of the receptor, demonstrating an IC50 value of 80 nM and a Ki of 28.67 nM. This compound has valuable applications in research focused on metabolic regulation and the development of therapeutic strategies for conditions such as obesity and diabetes. -
PPARγ Activator
Convallatoxin is a PPARγ activator derived from the plant Adonis amurensis. It exhibits significant anti-inflammatory effects by mitigating colitic inflammation through the activation of PPARγ and the suppression of NF-κB signaling pathways. Additionally, Convallatoxin serves as a substrate for P-glycoprotein, identifying Val982 as a critical amino acid for its transport. This compound also enhances ligand-induced micro-opioid receptor (MOR) endocytosis, demonstrating high potency and efficacy, making it valuable for research in inflammation and cellular signaling. -
PPAR-γ Activator
Glabrone, a PPAR-γ activator derived from the roots of Glycyrrhiza glabra, demonstrates notable ligand binding activity to this nuclear receptor. In addition to its role as a specific probe substrate for UGT1A9, Glabrone's metabolites inhibit neuraminidase, thus preventing influenza virus release. This compound is suitable for research applications focused on herb-drug interactions and the evaluation of anti-influenza viral activity. -
Anti-Inflammatory/Cancer Agent
Norathyriol is a natural metabolite derived from Mangifera, exhibiting significant anti-inflammatory and anticancer properties. It functions as a noncompetitive inhibitor of α-glucosidase with an IC50 value of 3.12 μM. Additionally, Norathyriol inhibits the peroxisome proliferator-activated receptors (PPARs) α, β, and γ, with IC50s of 92.8 μM, 102.4 μM, and 153.5 μM, respectively. This compound demonstrates a range of biological activities, including antioxidant, antimicrobial, and antibacterial effects, making it valuable for diverse research applications in inflammation and cancer therapeutics. -
PPARγ Activator/Mitochondrial Dysfunction Inducer
(S)-Coriolic acid is a potent PPARγ activator formed through the metabolism of linoleic acid by 15-lipoxygenase (15-LOX). This compound serves as a crucial intracellular signaling agent, influencing cell proliferation and differentiation across diverse biological systems. Additionally, (S)-Coriolic acid is known to induce mitochondrial dysfunction and contribute to airway epithelial injury, making it relevant for studies investigating cellular stress responses and respiratory health. -
PPARγ Inhibitor
PPARγ-IN-2 is a selective PPARγ inhibitor that effectively reduces triglyceride accumulation in 3T3-L1 preadipocytes, with an EC50 of 0.106 μM. This compound demonstrates potential for mitigating obesity and associated metabolic syndrome, particularly in the context of a high-cholesterol diet. Its ability to diminish lipid accumulation in adipose tissue makes it a valuable tool for research focused on metabolic disorders and adipocyte biology. -
PPARγ Activator
SDPC (DHA-PC) is a PPARγ activator that demonstrates significant anti-angiogenic properties. This phospholipid, featuring an ester bond with docosahexaenoic acid (DHA) at the sn-2 position, effectively inhibits the proliferation, migration, and tube formation of human umbilical vein endothelial cells. SDPC holds potential for applications in anti-tumor angiogenesis research, making it a valuable tool for studying tumor progression and vascular growth inhibition. -
PPARγ Agonist
AMG131 is a selective peroxisome proliferator-activated receptor γ (PPARγ) modulator, functioning as a potent non-thiazolidinedione (TZD) agonist. It binds to PPARγ in the same pocket as TZDs, yet interacts with the receptor at unique contact points, potentially leading to differential biological effects. This compound has significant potential for research applications related to type-2 diabetes mellitus and metabolic disorders. -
PPAR-δ Modulator
Bocidelpar is a selective PPAR-δ modulator that activates the PPAR-δ downstream signaling pathway, leading to the upregulation of target genes such as ABCA1 and ACAA2. This compound promotes fatty acid oxidation and enhances mitochondrial biogenesis, ultimately improving mitochondrial dysfunction. Bocidelpar is particularly useful in researching diseases associated with mitochondrial dysfunction, including primary mitochondrial myopathy (PMM) and Duchenne muscular dystrophy (DMD). -
FXR Antagonist
F44-A13 is a highly selective antagonist of the farnesoid X receptor (FXR), exhibiting an IC50 value of 1.1 μM. This compound modulates cholesterol metabolism by inducing the expression of CYP7A1, leading to significant reductions in cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C) in murine models. F44-A13 serves as a valuable tool for investigating metabolic diseases related to lipid dysregulation. -
PPARγ Antagonist
Mifobate is a potent antagonist of peroxisome proliferator-activated receptor gamma (PPARγ), selectively inhibiting thiazolidinedione (TZD)-induced transcriptional activity with an IC50 of 140 μM. This compound does not affect the basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR). Mifobate demonstrates significant antiobesity and antidiabetic effects, making it valuable for research applications aimed at exploring metabolic disorders and therapeutic interventions for related conditions. -
PPARγ Agonist
Leriglitazone hydrochloride is a potent agonist of the peroxisome proliferator-activated receptor gamma (PPARγ), with an EC50 of 9 μM. This compound is orally active and capable of penetrating the blood-brain barrier, exhibiting neuroprotective, anti-inflammatory, and antioxidant properties. Leriglitazone hydrochloride is suitable for research focused on neuroinflammatory and neurodegenerative diseases, providing valuable insights into mitochondrial function regulation. -
PPAR Agonist
Raspberry ketone is a potent PPAR-α agonist known for its role in lipid metabolism regulation. This naturally occurring aromatic compound, primarily derived from red raspberries, exhibits significant biological activity that may contribute to weight management and metabolic health research. Its applications extend to studying the effects on obesity and diabetes through modulation of lipid profiles and glucose homeostasis. -
PPAR Agonist
4-O-Methyl honokiol is a natural neolignan derived from Magnolia officinalis that functions as a selective PPARγ agonist. It exhibits significant inhibition of NF-κB activity, making it a valuable tool for studying mechanisms of inflammation and cancer. Its biological activity is particularly relevant in research focused on metabolic regulation and inflammatory responses. -
PPARγ inhibitor
SR 16832 is a dual-site covalent inhibitor of peroxisome proliferator-activated receptor gamma (PPARγ). It functions by targeting both orthosteric and allosteric sites, leading to significant modulation of PPARγ activity. This compound is valuable for research applications related to metabolic disorders, obesity, and diabetes, particularly in studies investigating the downstream effects of PPARγ inhibition on gene expression and cellular metabolism. -
PPAR-γ Agonist
Darglitazone is a thiazolidinedione and a potent, selective agonist of peroxisome proliferator-activated receptor gamma (PPAR-γ). It plays a significant role in the regulation of glucose homeostasis and lipid metabolism. Darglitazone is utilized in research focused on type II diabetes and related metabolic disorders, providing insights into its effects on insulin sensitivity and adipogenesis. -
PPARα Agonist
10-Hydroxystearic acid (10-HSA) is a PPARα agonist that promotes collagen synthesis. This compound exhibits significant anti-aging properties by enhancing skin texture, reducing the appearance of pores, and diminishing hyperpigmented lesions. 10-HSA is valuable for research focused on skin health, regenerative medicine, and dermatological studies. -
PPARα Activator
(10E,12Z)-Octadeca-10,12-dienoic acid is a potent PPARα activator that plays a critical role in regulating lipid metabolism and adipocyte differentiation. This compound has demonstrated various biological activities, including antioxidant and antitumor effects, alongside the induction of proinflammatory cytokines and chemokines, which may contribute to decreased adipogenesis and insulin resistance. (10E,12Z)-Octadeca-10,12-dienoic acid also influences milk fat synthesis by reducing the expression of lipogenic enzymes and inhibiting fatty acid desaturation. Additionally, it has been shown to modulate lipoprotein lipase activity in cultured adipocytes and alter hepatic stearoyl-CoA desaturase expression in vivo. -
PPARG Inhibitor
FTX-6746 is an orally active inhibitor of peroxisome proliferator-activated receptor gamma (PPARG). It demonstrates significant tumor inhibition in mouse xenograft models, making it a valuable tool for investigating the therapeutic potential of targeting PPARG in cancer research. Its specificity and efficacy in modulating PPARG activity support its use in studies related to metabolic disorders and cancer biology. -
PPARγ Inverse-Agonist
BAY-4931 is a selective inverse agonist of PPARγ, exhibiting potent action with an IC50 of 0.17 nM. This compound effectively modulates PPARγ activity, making it a valuable tool for investigating metabolic disorders and insulin sensitivity. Its unique mechanism of action allows for detailed studies of PPARγ's role in various biological processes and therapeutic applications. -
PPARβ/δ Inverse Agonist
ST247 is a potent inverse agonist of the peroxisome proliferator-activated receptor beta/delta (PPARβ/δ). It exhibits a high affinity for this target and modulates the expression of the activation marker CCL2 in a manner contrary to typical agonist activity. ST247 effectively promotes the interaction with corepressors and inhibits agonist-induced transcriptional activity of PPARβ/δ. This compound is valuable for research into metabolic disorders and inflammation, offering insights into the regulatory mechanisms mediated by PPARβ/δ. -
PPARγ Agonist
Edaglitazone is a selective and orally bioactive agonist of PPARγ, exhibiting an EC50 of 1053 nM for this target, alongside a lower affinity for PPARα at 35.6 nM. This compound demonstrates significant antidiabetic and anti-hyperglycemic properties, making it a valuable tool in diabetes research. Its ability to modulate metabolic pathways underscores its potential applications in studies related to glucose homeostasis and cardiovascular health. -
PPARα/γ Agonist
Saroglitazar magnesium is a selective agonist of peroxisome proliferator-activated receptors PPARα and PPARγ, exhibiting high potency with EC50 values of 0.65 pM and 3 nM, respectively, in HepG2 cells. This compound plays a crucial role in lipid metabolism and glucose homeostasis, making it a valuable tool for research in metabolic disorders such as dyslipidemia and type 2 diabetes. Its dual activity on PPARα and PPARγ positions it as a significant candidate for exploring therapeutic strategies in metabolic disease models. -
PPARδ Agonist
Mavodelpar is a selective PPARδ agonist that exerts protective effects against glomerular injury and renal fibrosis. This compound is particularly relevant in research focused on primary mitochondrial myopathies (PMM) and long-chain fatty acid oxidation disorders (LC-FAOD). Additionally, Mavodelpar features an alkyne functional group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) for click chemistry applications. -
PPARα Agonist
GW 590735 is a potent and selective PPARα agonist, exhibiting an EC50 of 4 nM with over 500-fold selectivity for PPARα compared to PPARδ and PPARγ. This compound is valuable for research focused on dyslipidemia and metabolic disorders, facilitating insights into lipid metabolism and potential therapeutic approaches targeting PPARα. -
PPAR Antagonist
H-Trp-Glu-OH is a selective and reversible antagonist of peroxisome proliferator-activated receptor gamma (PPARγ), with a dissociation constant (Kd) of approximately 8 µM. This compound has demonstrated cell permeability and presents potential as a lead compound in diabetes research. Its role in modulating PPARγ activity makes it an important tool for studying metabolic disorders and associated therapeutic pathways. -
PPARα Agonist
GW 9578 is a selective agonist of the peroxisome proliferator-activated receptor alpha (PPARα), exhibiting EC50 values of 5 nM for murine PPARα and 50 nM for human PPARα. This compound demonstrates significant lipid-lowering activity, making it a valuable tool for research in metabolic disorders and cardiovascular diseases. GW 9578 may be utilized in studies investigating the role of PPARα activation in lipid metabolism and related therapeutic applications. -
PPARγ Agonist
FK614 is a selective PPARγ modulator (SPPARM) that functions as a PPARγ agonist with significant anti-diabetic properties. This compound exhibits distinct effects on PPARγ activation throughout various stages of adipocyte differentiation. FK614 is utilized in research focused on hyperglycemia, hypertriglyceridemia, glucose intolerance, and type 2 diabetes, making it a valuable tool for understanding metabolic disorders.
