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Catalog No.
Product Name
Application
Product Information
Citations
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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 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. -
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 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. -
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. -
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. -
HSP Synthesis Inhibitor
KNK423 is a specific inhibitor of heat shock protein (HSP) synthesis, targeting HSP70. This compound enhances the efficacy of Amphotericin B against resistant strains of Aspergillus terreus by disrupting HSP expression. KNK423 is valuable for research in cancer therapy and bacterial infection mechanisms. -
FKBP51-Hsp90 Interaction Inhibitor
FKBP51-Hsp90-IN-1 is a selective inhibitor targeting the FKBP51-Hsp90 protein-protein interaction, exhibiting an IC50 value of 0.1 μM against FKBP51. This compound is valuable for research into stress-related diseases, Alzheimer's disease, and various metabolic disorders, owing to its ability to modulate protein interactions critical for cellular stress responses and stability. Its specificity makes it a potent tool for elucidating the role of FKBP51 in disease mechanisms. -
HSP90 Inhibitor
HSP90-IN-20 is a potent inhibitor of Heat Shock Protein 90 (HSP90) with an IC50 of ≤10 μM. This compound plays a significant role in cancer research by impeding the function of HSP90, which is critical for the stability and activity of several oncogenic proteins. HSP90-IN-20 can be utilized to investigate the therapeutic potential of HSP90 inhibition in various cancer models. -
HSP90 Inhibitor
Hsp90-IN-17 is a selective inhibitor of Heat Shock Protein 90 (HSP90) that interferes with its chaperone activity. This compound demonstrates significant potential in addressing various proliferative conditions, including cancer and neurodegenerative disorders. Hsp90-IN-17 serves as a valuable tool for research focused on the molecular mechanisms of HSP90 and its role in disease progression and treatment responses. -
HSP90 Inhibitor
Aminohexylgeldanamycin hydrochloride is a potent inhibitor of Heat Shock Protein 90 (HSP90). This Geldanamycin derivative demonstrates significant antiangiogenic and antitumor activities, making it valuable for cancer research. Its ability to modulate HSP90 function provides insights into the molecular mechanisms of tumorigenesis and offers potential therapeutic applications in oncology. -
SIRT2/Hsp70 Inhibitor
YM-08 is a selective inhibitor of SIRT2 and Hsp70, exhibiting an IC50 of 19.9 μM for SIRT2. This compound effectively penetrates the blood-brain barrier, making it a valuable tool for studying neurodegenerative diseases and cellular stress responses. Its dual inhibitory activity allows for investigation into SIRT2 and Hsp70's roles in various biological processes and potential therapeutic applications. -
HSP70 Inhibitor
DMT003096 is a selective inhibitor of HSP70, a heat shock protein that plays a critical role in cellular stress responses. Its upregulation has been associated with various cancers, including breast, lung, colon, and cervical cancer. This compound is valuable for research applications targeting cancer therapies and investigating the role of HSP70 in tumor progression and survival mechanisms. -
Hsp90 Inhibitor
Hsp90-IN-40 is a specific inhibitor targeting the C-terminal domain of heat shock protein 90 (Hsp90). It demonstrates significant antiproliferative activity against breast cancer cell lines SKBr3 and MCF-7, with IC50 values of 2.57 µM and 2.43 µM, respectively. By disrupting the function of Hsp90, Hsp90-IN-40 promotes the degradation of Hsp90-dependent proteins, thereby inhibiting cancer cell growth. This compound is valuable for research applications focusing on breast cancer therapeutics and mechanisms of Hsp90 inhibition. -
HSP90 Inhibitor
STA-1474 is a potent and selective inhibitor of Heat Shock Protein 90 (HSP90), primarily functioning by disrupting its chaperone activities, which are crucial for the stability and function of numerous oncogenic proteins. This compound induces apoptosis in tumor cells and exhibits significant antitumor efficacy in spontaneous canine cancer models, such as osteosarcoma and thyroid carcinoma. STA-1474 is valuable for research on solid tumors, including osteosarcoma and breast cancer, and offers insights into the role of HSP90 in cancer biology. -
Hsp90 Inhibitor
Hsp90-IN-15 is a potent Hsp90 inhibitor that exhibits significant anticancer activity. This compound promotes apoptosis in cancer cells and effectively induces cell cycle arrest at the S phase. Hsp90-IN-15 also reduces the expression levels of Hsp90 in HeLa cells, making it a valuable tool for research into cancer therapies targeting the Hsp90 chaperone pathway. -
HSP90 Inhibitor
Hsp90-IN-38 is a potent inhibitor of heat shock protein 90 (HSP90), displaying a strong binding affinity with a dissociation constant (Kd) of 87 nM. This compound effectively inhibits HSP90 ATPase activity, with an IC50 of 0.13 μM. Biological activity has been demonstrated in various cancer cell lines, including HCT116, MCF-7, SKBr3, K562, and A549, with reported IC50 values of 0.187, 0.072, 0.105, 0.403, and 0.31 μM, respectively. Hsp90-IN-38 serves as a valuable tool for research into cancer biology and HSP90-related pathways. -
Hsp90 Inhibitor
PU-20F is a potent Hsp90 inhibitor characterized by an EC50 value of 6.8 μM. This compound competes with Geldanamycin for binding to Hsp90, effectively regulating the activity of this crucial molecular chaperone. PU-20F promotes the degradation of the oncogenic Her2 tyrosine kinase and has demonstrated the ability to inhibit the proliferation of breast cancer cells. It serves as a valuable tool for research focused on breast cancer biology and therapeutic strategies.
