Catalog No.
Product Name
Application
Product Information
Citations
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Endogenous Metabolite
9,10-EpOME (9,10-Epoxyoctadecenoic acid) is a cytochrome P450-derived metabolite of linoleic acid. It is known to induce oxidative stress by activating the NF-κB and AP-1 transcription factors and facilitates the chemotaxis of human neutrophils. Additionally, 9,10-EpOME has been shown to induce mechanical and thermal pain in wild-type mice via the PKA pathway. This compound is useful for investigating mechanisms of inflammation and pain in research settings. -
Ferroptosis/DNA Damage Inducer
HJ03 is a potent inducer of ferroptosis that targets DNA damage pathways. It enhances intracellular reactive oxygen species (ROS) levels, facilitates Fe2+ accumulation, and promotes lipid peroxidation, ultimately leading to the induction of DNA adducts and interstrand crosslinks. By inhibiting DNA replication and transcription, HJ03 effectively arrests the cell cycle at the G2/M phase and triggers apoptosis. This reagent is valuable for investigating glioblastoma multiforme and colorectal cancer research. -
AHR Agonist
AHR Agonist 10 is a potent agonist of the aryl hydrocarbon receptor (AHR), exhibiting an EC50 of 2.01 nM. This compound significantly upregulates the expression of AHR downstream target genes, such as CYP1A1 and CYP1B1, while downregulating pro-inflammatory markers including CD36, IL-18, CCL5, CCL20, IL-6, and TNF-α. AHR Agonist 10 demonstrates low cytotoxicity (above 40 μM) in normal cells, making it suitable for use in psoriasis research and studies investigating AHR-dependent modulation of inflammatory responses. -
AHR Agonist
PY109 is a highly selective aryl hydrocarbon receptor (AHR) agonist that exhibits oral bioactivity. It demonstrates potent efficacy with EC50 values of 1.2 nM in human HepG2 cells and 1.4 nM in mouse Hepa-1c1c7 cells. PY109 significantly enhances the expression of CYP1A1 and interleukin-22 (IL-22), while inhibiting interleukin-17A (IL-17A) expression. This compound has been shown to effectively improve colitis in murine models, making it a valuable tool for research focused on inflammatory bowel diseases. -
Cathepsin L Inhibitor
Cathepsin L-IN-6 is a selective inhibitor of cathepsin L, exhibiting an IC50 value of 0.021 μM. It functions by directly binding to cathepsin L, effectively suppressing its enzymatic activity. Additionally, Cathepsin L-IN-6 inhibits pro-inflammatory cytokines IL-6 and IL-8, demonstrating significant anti-inflammatory properties. This compound is particularly relevant for research focused on acute lung injury and related inflammatory conditions. -
HSP90α Inhibitor
HSP90α-IN-1 is a selective inhibitor of HSP90α, with an IC50 value of 111 nM, demonstrating significant senolytic activity in diverse cellular senescence models. This compound is associated with the xanthinic family and plays a critical role in investigations aimed at addressing age-related inflammaging and associated diseases, including cancer. HSP90α-IN-1 is also being explored for its potential to promote healthy lifespan extension in various biological research contexts. -
PDE4 Inhibitor
Etazolate is a selective phosphodiesterase 4 (PDE4) inhibitor that exhibits anti-inflammatory properties by reducing interleukin-1 beta (IL-1β) levels. This compound demonstrates a dose-dependent effect on inflammation and edema, while also contributing to enhanced memory performance. Additionally, Etazolate's modulation of GABAA receptors suggests potential applications in research related to mood disorders, particularly in studying antidepressant-like effects. -
PKM2 Inhibitor
LIQ1 is a potent allosteric inhibitor of Pyruvate kinase M2 (PKM2), targeting Arg43 within the polyarginine pocket with an IC50 of 0.39 μM and a Kd of 4.5 μM. This flavonoid derivative effectively prevents the nuclear translocation of PKM2 and its interaction with HIF-1α, leading to the suppression of IL-1β transcription. LIQ1 is valuable for research involving endotoxemic conditions, particularly in studies of inflammation and metabolic regulation. -
PDE4 Inhibitor
PDE4-IN-8 is a potent inhibitor of phosphodiesterase 4 (PDE4), demonstrating an IC50 of 0.93 nM specifically for the PDE4B2 isoform. This compound exhibits selective inhibition, with minimal effects on cytokines such as IL-13 (IC50 = 4.04 nM), IL-4 (IC50 = 36.33 nM), and IFN-γ (IC50 = 2394 nM). PDE4-IN-8 is suitable for research applications focused on inflammation and other PDE4-related pathways in various biological contexts. -
PDE3A/PDE4B Inhibitor
PDE3/4-IN-4 is a potent and selective inhibitor of phosphodiesterase 3A (PDE3A) and phosphodiesterase 4B (PDE4B), exhibiting IC50 values of 10 nM and 9.4 nM, respectively. This compound modulates the cAMP/PKA/CREB signaling pathway, effectively inhibiting the pro-inflammatory cytokine IL-6 and reducing expression of inflammatory markers in liver tissue. PDE3/4-IN-4 demonstrates potential in mitigating liver fibrosis and limiting liver damage in models of cholestatic and sepsis-induced liver diseases. This reagent is suitable for research focused on liver injury and cholestatic liver disorders. -
Hsp90 Inhibitor
Pochonin D ((+)-Pochonin D) is a potent inhibitor of heat shock protein 90 (Hsp90) with demonstrated antiviral and anti-inflammatory activities. By targeting Hsp90, Pochonin D disrupts the proper folding, stabilization, and assembly of client proteins, including viral proteins, thereby impairing viral protein homeostasis and significantly reducing viral replication capacity. In addition, Pochonin D exhibits anti-inflammatory effects by attenuating inflammatory cell infiltration and suppressing the production of pro-inflammatory cytokines, such as TNF-α and IL-1β. These combined pharmacological properties highlight Pochonin D as a promising small-molecule tool for the study of human rhinovirus (HRV) infection and cancer-related pathways.
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PFKFB4 Inhibitor
5MPN is a selective inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4), exhibiting competitive inhibition at the fructose-6-phosphate binding site with a Ki of 8.6 μM. This compound does not affect PFK-1 or PFKFB3, allowing for targeted modulation of glucose metabolism in cancer cells. 5MPN has demonstrated the ability to suppress the proliferation of various human cancer cell lines, making it a valuable tool for research in cancer metabolism and therapeutic development. -
PTP1B Inhibitor
Caffeoyltryptophan is a competitive inhibitor of protein tyrosine phosphatase 1B (PTP1B), exhibiting an IC50 of 16.99 μM. Additionally, it demonstrates inhibitory effects on α-glucosidase, linoleic acid peroxidation, and hemolysis. This compound is primarily utilized in research related to type 2 diabetes, offering insights into metabolic regulation and potential therapeutic avenues. -
FXR Agonist
EDP-305 is a highly selective agonist of the farnesoid X receptor (FXR), exhibiting potent activity with EC50 values of 34 nM in chimeric FXR and 8 nM in full-length FXR. This compound demonstrates significant antifibrotic effects, making it a valuable tool for studying liver diseases. EDP-305 is relevant in research focused on primary biliary cholangitis (PBC) and non-alcoholic steatohepatitis (NASH). -
PFKFB3 Inhibitor
PFKFB3-IN-2 is a selective inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3). It demonstrates key biological activity by modulating glucose metabolism, making it relevant in cancer research and neurodegenerative disorders. This compound holds potential for applications in autoimmune diseases, inflammatory conditions, multiple sclerosis, metabolic disorders, and the study of angiogenesis. -
DPP-4 Inhibitor
Antidiabetic agent 2 is a potent DPP-4 inhibitor that effectively promotes glucose uptake. This compound also inhibits PTP-1B, α-amylase, and α-glucosidase, exhibiting IC50 values of 0.036, 0.042, 0.241, and 0.185 μM, respectively. By decreasing blood glucose levels, Antidiabetic agent 2 serves as a valuable tool for research focused on diabetes management and the modulation of glucose homeostasis. -
Ethyl Caffeoylquinate
Ethyl-3,5-di-O-caffeoylquinate is a derivative of ethyl caffeoylquinate, primarily targeting α-glucosidase and PTP1B enzymes. This compound demonstrates potential as an inhibitor of these critical enzymes, making it valuable for research in metabolic disorders and diabetes management. Isolated from the flower buds of Lonicera macranthoides, it also serves as an isomer of chlorogenic acid (ethyl dicaffeoylquinate), expanding its relevance in phytochemical studies and pharmacological applications. -
Phosphatase Inhibitor
Chrysophanol triglucoside is an anthraquinone with a specific inhibitory action on protein tyrosine phosphatase 1B (PTP1B) and α-glucosidase, demonstrating IC50 values of 80.17 µM and 197.06 µM, respectively. This compound is derived from Cassia obtusifolia and has potential applications in diabetes research, particularly in the study of glucose metabolism and insulin signaling pathways. -
Prenylated Flavonoid
Parvisoflavone B is a prenylated flavonoid that selectively inhibits protein tyrosine phosphatase 1B (PTP1B) with an IC50 of 42.6 μM and α-glucosidase with an IC50 of 12.19 μM. This compound is derived from the root bark of Erythrina mildbraedii and exhibits significant biological activity relevant to metabolic disorders. Parvisoflavone B is utilized in research exploring mechanisms related to type 2 diabetes and obesity, making it a valuable tool for studying these conditions. -
Carbonic Anhydrase/Alkaline Phosphatase Inhibitor
ALP/Carbonic Anhydrase-IN-1 is a dual inhibitor of carbonic anhydrase (CA) and alkaline phosphatase (ALP), selectively targeting key isoforms. It demonstrates IC50 values of 0.44 µM for CA-II, 1.61 µM for CA-IX, 0.51 µM for CA-XII, and 0.107 µM for ALP, indicating potent inhibitory activity. This compound is useful in exploring the roles of carbonic anhydrase and alkaline phosphatase in various biological processes and disease models. -
Bipyridine Herbicide
Morfamquat dichloride is a bipyridine herbicide that primarily targets the reticuloendothelial system. It induces significant lysosomal membrane damage and enzyme leakage, disrupting the function of the hepatocyte Golgi apparatus and associated glucose metabolic pathways. Research has shown that Morfamquat dichloride increases the activities of acid phosphatase and β-glucuronidase, resulting in toxic effects in mice; however, pre-administration of vitamin E has been observed to mitigate these toxic effects. This compound is relevant for studies investigating herbicide mechanisms and the associated biochemical responses in metabolic systems. -
PTP1B/hMAO-A Inhibitor
Cassiaside B2 is an inhibitor of protein tyrosine phosphatase 1B (PTP1B) and human monoamine oxidase A (hMAO-A). This compound exhibits significant antiallergic properties and functions as a 5-HT2C receptor agonist. It serves as a valuable tool for understanding the modulation of these targets in various biological pathways and contributes to research in neuropharmacology and allergy-related studies. -
PFKFB3 Inhibitor
(E/Z)-3PO is a selective inhibitor of PFKFB3, a key regulator of glycolysis. This compound effectively inhibits glycolysis, reduces the extracellular acidification rate, and suppresses angiogenesis by impairing endothelial cell migration and capillary tube formation. Research applications of (E/Z)-3PO include investigations into cancer, acute lung injury, pulmonary fibrosis, and atherosclerosis, making it a valuable tool for exploring therapeutic strategies in these diseases. -
Endogenous Metabolite
Glycodeoxycholic Acid is an endogenous metabolite that plays a significant role in hepatic physiology. It has been shown to induce hepatocyte necrosis and initiate autophagy, particularly in conditions such as obstructive cholestasis. This compound is essential for studying liver pathology and can be utilized in research focused on cholestatic liver diseases and cellular response mechanisms. -
Hsp110-STAT3 Interaction Inhibitor
Hsp110-STAT3 PPI-IN-1 is a potent inhibitor of the Hsp110-STAT3 protein-protein interaction. This compound exhibits antiproliferative activity against the HPAEC cell line, demonstrating an IC50 value of 22.67 μM. It serves as a valuable tool for investigating the role of Hsp110-STAT3 interactions in various biological processes and therapeutic applications. -
HMG-CoA Inhibitor
HMG499 is a potent and selective inhibitor of HMG-CoA reductase, exhibiting an IC50 of 0.41 μM. This compound effectively reduces serum cholesterol levels and mitigates the statin-induced accumulation of HMGCR, making it a valuable tool for research in lipid metabolism and atherosclerosis. HMG499 is relevant for studies investigating cholesterol regulation and cardiovascular disease pathways. -
Cathepsin Inhibitor
LV-320 is a potent uncompetitive inhibitor of cathepsin ATG4B, exhibiting an IC50 of 24.5 μM and a Kd of 16 μM. This compound effectively inhibits the enzymatic activity of ATG4B, thereby obstructing autophagic flux in cellular environments. Due to its stability and low toxicity, LV-320 is suitable for in vivo applications, making it a valuable tool for research on autophagy-related pathways. -
Nampt Inhibitor
GPP78 is a potent inhibitor of nicotinamide adenine dinucleotide (NAD) biosynthesis via the enzyme Nampt, demonstrating an IC50 of 3.0 nM. It exhibits cytotoxicity in the neuroblastoma SH-SY5Y cell line, with an IC50 of 3.8 nM, primarily by inducing autophagy. GPP78 serves as a valuable tool in cancer and inflammatory research, highlighting its potential therapeutic applications in oncology. -
RXR Agonist
Bexarotene-d4 is a deuterium-labeled analog of Bexarotene, functioning as a selective retinoid X receptor (RXR) agonist. This compound is primarily utilized in the treatment of cutaneous T-cell lymphoma, demonstrating significant biological activity in modulating RXR signaling pathways. Its isotopic labeling facilitates research applications in pharmacokinetics and metabolism studies of RXR-targeted therapies. -
HMG-CoA Reductase Inhibitor
Atorvastatin hemicalcium trihydrate is an orally active inhibitor of HMG-CoA reductase, primarily utilized in the management of dyslipidemia by effectively lowering blood lipid levels. Additionally, it demonstrates inhibitory effects on human smooth muscle cell proliferation and invasion, with IC50 values of 0.39 μM and 2.39 μM, respectively. This compound is valuable for research focused on atherosclerosis, cardiovascular diseases, and cell growth regulation. -
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. -
PDEδ Autophagic Degrader
PDEδ autophagic degrader 1 is a targeted autophagic degrader of PDEδ, functioning through an autophagosome-tethering mechanism. This compound effectively reduces the levels of PDEδ protein via lysosome-mediated autophagy, while leaving PDEδ mRNA expression unchanged. Its ability to suppress growth in KRAS mutant pancreatic cancer cells highlights its potential applications in cancer research and therapeutic development. -
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. -
FXR Agonist
Cilofexor tromethamine is a nonsteroidal agonist of the farnesoid X receptor (FXR), primarily targeting liver diseases. It demonstrates significant potential in improving markers of cholestasis and liver injury, making it a valuable reagent in research for conditions such as primary sclerosing cholangitis. Cilofexor tromethamine has exhibited a favorable safety profile in clinical studies involving patients without cirrhosis, leading to notable enhancements in liver biochemical parameters and cholestatic markers. -
RAR/RXR
Ch55-O-C3-NH2 is a selective ligand for retinoic acid receptors (RAR) and retinoid X receptors (RXR). This compound demonstrates the ability to effectively modulate RAR signaling pathways, facilitating research into their role in gene expression and developmental processes. Ch55-O-C3-NH2 can also be utilized in the synthesis of SNIPERs by binding to cIAP1 ligand Bestatin through a linker, supporting studies in targeted protein degradation and therapeutic applications. -
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. -
NAMPT Degrader
NAMPT degrader-1 is an autophagosome-tethering compound (ATTEC) that targets nicotinamide phosphoribosyltransferase (NAMPT) with an IC50 of 0.023 μM. This compound effectively induces the degradation of NAMPT via the autophagy-lysosomal pathway, demonstrating significant antitumor activity in cellular models. NAMPT degrader-1 is valuable for research focused on cancer biology and the regulation of metabolic pathways involving NAD+ synthesis. -
PPAR Activator
Rosiglitazone sodium is a potent and selective activator of the peroxisome proliferator-activated receptor gamma (PPARγ), exhibiting EC50 values of 30 nM, 100 nM, and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, with a Kd of approximately 40 nM. In addition to its role as a PPARγ activator, Rosiglitazone sodium functions as a modulator of transient receptor potential (TRP) channels, specifically inhibiting TRP melastatin 2 (TRPM2) and TRPM3, while activating TRP canonical 5 (TRPC5). This compound is utilized in research related to metabolic disorders, obesity, and other conditions linked to PPARγ signaling. -
RAR/RXR Agonist
Acitretin sodium functions as a retinoic acid receptor (RAR) and retinoid X receptor (RXR) agonist. Primarily utilized in the treatment of psoriasis, this second-generation systemic retinoid also shows potential in the research of Alzheimer's disease. Its ability to modulate gene expression and influence cellular differentiation makes it a valuable tool for investigating retinoid signaling pathways in various biological contexts. -
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 B Substrate
Z-Arg-Arg-AMC hydrochloride is a selective substrate for the cysteine protease cathepsin B. This compound is utilized in biochemical assays to monitor cathepsin B activity, making it essential for studying cellular processes such as protein degradation and apoptosis. Its application extends to cancer research and investigations into various diseases where cathepsin B is implicated. -
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.
