Catalog No.
Product Name
Application
Product Information
Citations
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DHFR Inhibitor
DHFR-IN-3 is a dihydrofolate reductase (DHFR) inhibitor that demonstrates an IC50 of 19 μM in rat liver DHFR and 12 μM in P. carinii DHFR. This compound is primarily utilized in pharmacological research to study the role of DHFR in folate metabolism and its implications in various disease states, including cancer and parasitic infections. Its inhibitory activity makes it a valuable tool for investigating potential therapeutic strategies targeting DHFR-related pathways. -
Drug Metabolite
Desmethyl ferroquine is the primary active metabolite of Ferroquine, targeting malaria infection. It exhibits significant antimalarial activity against both Chloroquine-susceptible and resistant strains of Plasmodium falciparum. This compound is valuable for research applications focused on malaria treatment and drug resistance mechanisms. -
DHFR Inhibitor
Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor primarily utilized in antimalarial research. It is metabolized into the active compound Cycloguanil, which demonstrates significant efficacy against Plasmodium species. This reagent is essential for studies focused on antimalarial drug development and exploration of DHFR pathways in cellular metabolism. -
TbNMT Inhibitor
NMT-IN-1 is an inhibitor of Trypanosoma brucei N-myristoyltransferase (TbNMT) with an IC50 of 31 μM, demonstrating selectivity over human N-myristoyltransferase (hNMT) with an IC50 of 66 μM. This thiazolidinone compound acts by binding to the active site of TbNMT, effectively inhibiting the myristoyl transfer reaction catalyzed by the enzyme. NMT-IN-1 is valuable in research focused on developing anti-parasitic agents for human African trypanosomiasis (African sleeping sickness) and serves as a structural foundation for optimizing TbNMT inhibitors with improved efficacy and selectivity for therapeutic applications. -
Fungal Metabolite
Paraherquamide E is a fungal metabolite derived from Penicillium charlesii, targeting nematodes and parasites. It exhibits significant antinematodal and antiparasitic activity, making it a valuable reagent for research in parasitology and agricultural science. Its biological properties can aid studies on the mechanisms of action against parasitic infections and nematode control strategies. -
Small-molecule Pheromone
Ascr#9 is a small-molecule pheromone from the ascaroside family, primarily targeting nematodes. It induces dispersal and avoidance behaviors in species such as Caenorhabditis elegans and entomopathogenic nematodes, indicating its role in prompting movement away from unfavorable conditions. Additionally, Ascr#9 demonstrates repellent activity against Meloidogyne incognita, making it a valuable tool for research on nematode behavior and ecology. -
PfGSK3/PfPK6 Inhibitor
PfGSK3/PfPK6-IN-1 is a selective inhibitor targeting PfGSK3 and PfPK6, with IC50 values of 97 nM and 8 nM, respectively. This compound effectively inhibits the proliferation of blood-stage Plasmodium falciparum 3D7 parasites, making it a valuable tool for malaria research. Additionally, PfGSK3/PfPK6-IN-1 exhibits low cytotoxicity in hepatocyte cultures at concentrations up to 200 nM, with a significant reduction in cell viability observed at 2 μM. Its dual action enhances its potential in studying malaria-related mechanisms and potential therapeutic strategies. -
CYP3A4 Inhibitor
SR9186 is a selective inhibitor of CYP3A4, demonstrating potent inhibition with IC50 values of 9 nM for the metabolism of Midazolam, 4 nM for Testosterone, and 38 nM for Vincristine. This compound effectively impedes hepatic-stage P. falciparum development and obstructs the metabolism of ivermectin. Its utility extends to breast cancer research, making it a valuable tool for investigating drug metabolism and therapeutic applications. -
Insect Pheromone
(Z,E)-9,12-Tetradecadienol is a synthetic insect pheromone that enhances the attraction of male Ephestia cautella. This compound plays a crucial role in insect behavioral research, facilitating the study of mating patterns and chemical communication in Lepidoptera. Its application extends to pest management strategies and ecological studies, making it a valuable reagent for researchers in entomology and pheromone dynamics. -
N-myristoyltransferase Inhibitor
IMP-1002 is an inhibitor of N-myristoyltransferase (NMT) in Plasmodium species. By inhibiting myristoylation activity, IMP-1002 effectively blocks the development of the malaria parasite. This reagent is suitable for research applications aimed at understanding malaria pathology and exploring novel therapeutic strategies. -
trans-cinnamic acid Derivative
trans-2-Methoxycinnamic acid is a derivative of trans-cinnamic acid that primarily targets α-glucosidase. This compound exhibits inhibitory activity with an IC50 of 4.34 mM. It is relevant for research applications involving HIV infection and hyperglycemia, making it a valuable tool for studying metabolic disorders and viral pathogenesis. -
Endogenous Metabolite
8-Oxo-dATP lithium is an oxidized purine nucleoside triphosphate that targets the MTH1 enzyme. This compound plays a crucial role in cellular metabolism by being hydrolyzed into monophosphates, which effectively prevents the misincorporation of 8-oxo-dATP during DNA replication and transcription processes. It is applicable in research concerning oxidative stress, DNA damage repair mechanisms, and the fidelity of nucleotide incorporation in cellular systems. -
Fungal Metabolite
3α,11β,21-Trihydroxy-20-oxo-5β-pregnan-18-al is a fungal metabolite known for its role in biological processes associated with gut fungi. This compound exhibits various biological activities that contribute to the understanding of fungal metabolism and its impact on human health. It serves as a valuable research tool in studies investigating the interactions between gut microbiota and host physiology. -
MAO Inhibitor
9-Methyl-β-carboline is a potent monoamine oxidase (MAO) inhibitor, demonstrating an IC50 of 1 μM for human MAO-A and 15.5 μM for human MAO-B. This compound shows significant potential for cognitive enhancement by increasing dopamine levels through its inhibition of MAO activity and modulation of microglial proliferation. Additionally, 9-Methyl-β-carboline activates signaling pathways such as PKA/PKC and influences mitochondrial respiratory function, contributing to neuroprotection and the reduction of α-synuclein levels. It is particularly relevant in research focusing on Parkinson's disease, given its neurotrophic effects and ability to counteract neurotoxin-induced dopaminergic neuron damage. -
Drug Metabolite
Deacetylmoxisylyte is an orally active drug metabolite derived from the prodrug Moxisylyte, primarily targeting alpha-1 and alpha-2 adrenoceptors. It demonstrates significant affinity and selectivity in rabbit corpus cavernosum and urethra tissues, with IC50 values of 400 nM and 1200 nM, respectively. This compound is valuable in pharmacological research focused on understanding adrenergic receptor interactions and their physiological effects. -
Endogenous Metabolite
Amylin (IAPP), feline is a 37-amino acid polypeptide that serves as an endogenous metabolite derived from feline sources. This regulatory peptide is primarily secreted by the β-cells of the pancreatic islets, where it plays a crucial role in glucose homeostasis by inhibiting the secretion of insulin and glucagon. Its unique biological activity makes it a valuable tool for research on metabolic disorders and endocrine function in feline models. -
GRP/BN receptor Antagonist
BIM-26226 is a selective antagonist of the gastrin-releasing peptide receptor (GRPR) and bombesin (BN) receptor, exhibiting an IC50 of 6 nM. This compound effectively inhibits BN- or GRP-stimulated amylase release with IC50 values of 0.3 nM and 0.2 nM, respectively. BIM-26226 shows high specificity for the GRP-preferring BN receptor subtype and does not interfere with the GRP receptor system. Additionally, it can induce the synthesis of somatostatin receptors while demonstrating no significant effect on tumor growth, making it valuable for research into neuropeptide signaling and related biological pathways. -
GRP/Bombesin Receptor 2 Antagonist
ICI 216140 is a potent GRP/bombesin receptor 2 antagonist with an IC50 value of 2 nM. This compound effectively inhibits Bombesin-stimulated pancreatic amylase secretion and mitigates Bombesin-induced increases in blood pressure. ICI 216140 is valuable for research into the physiological roles of bombesin receptors and their implications in various pathophysiological conditions. -
Bombesin Receptor Antagonist
[D-Phe12]-Bombesin is a bombesin receptor antagonist with a Ki value of 4.7 μM. This compound effectively inhibits bombesin-induced amylase release, exhibiting an IC50 of 4 μM. It is valuable for research applications exploring the role of bombesin receptors in physiological and pathological processes, particularly in studies related to neuroendocrine signaling and cancer biology. -
CB2R/FAAH Modulator
CB2R/FAAH modulator-3 is a dual-targeting compound that functions as an agonist of the cannabinoid receptor type 2 (CB2R) and an inhibitor of fatty acid amide hydrolase (FAAH). It exhibits Ki values of 20.1 nM for CB2R and 67.6 nM for CB1R, with an IC50 of 3.4 μM for FAAH. This modulator is valuable for research into cancer biology, inflammatory processes associated with neurodegenerative diseases, and potential therapeutic approaches for COVID-19. -
CB/FAAH Inhibitor
Isopropyl dodec-11-enylfluorophosphonate (IDEFP) is a potent inhibitor of the central cannabinoid receptor (CB1) and fatty acid amide hydrolase (FAAH), exhibiting similar inhibitory activities with IC50 values around 2 nM. It serves as a valuable tool for investigating cannabinoid signaling pathways and lipid metabolism in various biological contexts. Researchers utilize IDEFP to explore the therapeutic potential of modulating endocannabinoid systems in pain, inflammation, and neuroprotection studies. -
CETP Inhibitor/CB1 Agonist
BI-5756 is a selective CETP inhibitor and cannabinoid receptor 1 (CB1) agonist. It promotes a significant increase in HDL-C levels while reducing LDL-C levels, thereby improving lipid profiles. Additionally, BI-5756 enhances the function of regulatory T cells and preserves T cell-mediated anti-tumor activity, exhibiting direct anti-proliferative effects on tumor cells. This compound also upregulates the expression of MHC I, MHC II, and CD80 on tumor cells and demonstrates protective effects in graft-versus-host disease. BI-5756 is applicable in research related to oncology, graft-versus-host disease, and metabolic disorders. -
CB2R/FAAH Modulator
CB2R/FAAH modulator-2 is a dual-targeting modulator that functions as an agonist of the cannabinoid receptor 2 (CB2R) and an inhibitor of fatty acid amide hydrolase (FAAH). It exhibits Ki values of 10.8 nM for CB2R and 152.9 nM for CB1R, with an IC50 of 6.2 μM for FAAH. This compound is suitable for investigating therapeutic applications in cancer, neurodegenerative diseases characterized by inflammatory processes, and potential impacts on COVID-19 infection pathways. -
CB2R Agonist/FAAH Inhibitor
CB2R/FAAH modulator-1 is a potent full agonist of the cannabinoid type 2 receptor (CB2R), exhibiting a binding affinity with a Ki of 14.8 nM for CB2R and 241.3 nM for CB1R. This compound also serves as an inhibitor of fatty acid amide hydrolase (FAAH), demonstrating an IC50 of 4 μM. CB2R/FAAH modulator-1 is effective in modulating cytokine production by decreasing pro-inflammatory cytokines while enhancing anti-inflammatory cytokine levels, making it valuable for research in inflammation and pain modulation. -
Endogenous Metabolite
Phosphorylcholine, an endogenous metabolite, is a key component of many biological membranes, particularly in eukaryotic cells. It plays a crucial role in cell signaling and immune modulation, influencing both the host and microbial interactions in the microbiome. Due to its diverse immunomodulatory properties, phosphorylcholine is valuable in research applications related to immunology, microbiology, and cell biology. -
Endogenous Metabolite
Phosphorylcholine chloride is an endogenous metabolite primarily involved in the formation of phospholipid membranes in eukaryotic biofilms. Found in both commensal and pathogenic bacteria, it plays a crucial role in host-microbe interactions. This compound exhibits diverse immunomodulatory effects, making it valuable for research in immunology and cellular signaling pathways. -
SREBPs/microRNA 33a/b Inhibitor
Pseudoprotodioscin is a furostanoside that inhibits Sterol Regulatory Element-Binding Proteins (SREBPs) and microRNA 33a/b. This inhibition leads to a reduction in the gene expression involved in cholesterol and triglyceride synthesis. Pseudoprotodioscin is valuable for research on lipid metabolism and related cardiovascular diseases. -
AhR Agonist
Norisoboldine hydrochloride is an orally active agonist of the aryl hydrocarbon receptor (AhR). This natural isoquinoline alkaloid, predominantly found in Radix Linderae, demonstrates significant biological activity relevant to inflammatory disorders. It is particularly valuable for research related to rheumatoid arthritis and ulcerative colitis. -
A2AAR/hMAO-B Inhibitor
A2AAR/hMAO-B-IN-1 is a non-xanthine dual-target inhibitor that selectively inhibits the A2A adenosine receptor (A2AAR) with an IC50 of 34.9 nM, and human monoamine oxidase B (MAO-B) with a Ki of 39.5 nM. The compound effectively disrupts A2AAR-mediated cAMP accumulation and demonstrates competitive, reversible inhibition of MAO-B. A2AAR/hMAO-B-IN-1 is suitable for research applications in neurodegenerative diseases, particularly in the study of Parkinson's disease (PD). -
Endogenous Metabolite
Phenylpyruvic acid sodium is an endogenous metabolite that acts primarily as a precursor in the synthesis of 3-phenyllactic acid via lactate dehydrogenase. It exhibits notable antifungal properties, enhancing the activity of multiple lactic acid bacterial strains against fungal contaminants such as Aspergillus niger and Penicillium roqueforti. Additionally, phenylpyruvic acid sodium influences enzymatic activity in the pentose phosphate pathway, notably reducing glucose-6-phosphate dehydrogenase activity in rat brain homogenates, making it a valuable reagent for research in metabolic and antifungal studies. -
Endogenous Metabolite
Nicotinamide riboside malate is an endogenous metabolite that acts as an orally active precursor of NAD+. This compound is known to elevate NAD+ levels and activate sirtuin enzymes SIRT1 and SIRT3, playing a crucial role in enhancing oxidative metabolism. Additionally, nicotinamide riboside malate has demonstrated protective effects against metabolic disorders induced by high-fat diets and mitigates cognitive decline in transgenic mouse models of Alzheimer’s disease. It serves as a valuable tool for research into metabolic health and neurodegeneration. -
Endogenous Metabolite
Nicotinamide riboside tartrate serves as an orally bioavailable precursor of NAD+, primarily targeting the enhancement of NAD+ levels. It activates sirtuins SIRT1 and SIRT3, contributing to increased oxidative metabolism and protection against metabolic disturbances linked to high-fat diets. In preclinical studies, nicotinamide riboside tartrate has demonstrated potential in mitigating cognitive decline in transgenic mouse models of Alzheimer’s disease, underscoring its relevance in neurodegenerative research and metabolic health exploration. -
CypD Inhibitor
CypD-IN-5 is a selective inhibitor of cyclophilin D (CypD), a key regulator of mitochondrial permeability transition. This compound demonstrates significant potential in modulating mitochondrial function and may be particularly useful in studying neurodegenerative diseases such as Alzheimer's disease. Its application in research focuses on understanding the role of CypD in cellular stress responses and the underlying mechanisms of neurodegeneration. -
PNMT Inhibitor
1-(2,3-Dichlorophenyl)ethanamine hydrochloride is a selective inhibitor of phenylethanolamine N-methyltransferase (PNMT). This compound effectively lowers blood pressure in spontaneously hypertensive models, making it a valuable tool for studying hypertension and its mechanisms. Researchers can utilize 1-(2,3-Dichlorophenyl)ethanamine hydrochloride to investigate the role of PNMT in blood pressure regulation and explore potential therapeutic avenues for hypertensive disorders. -
MAO Inhibitor
Harmane hydrochloride is a monoamine oxidase (MAO) inhibitor that exhibits multiple biological activities. It demonstrates significant inhibition of MAO-A and MAO-B, with IC50 values of 0.5 μM and 5 μM, respectively. This compound has been shown to possess antidepressant, anti-anxiety, anticonvulsant, and analgesic properties, making it valuable in neuropharmacological research. Additionally, Harmane hydrochloride can influence tyrosine hydroxylase activity, impacting dopamine biosynthesis and enhancing cytotoxicity induced by L-DOPA in in vitro models. Its mutagenic potential is also notable, particularly in conjunction with 2-acetylaminofluorene. -
PNMT Inhibitor
LY 78335 is a potent inhibitor of phenylethanolamine-N-methyltransferase (PNMT) with a Ki value of 0.09 μM. This compound also functions as an α₂-adrenoceptor antagonist, exhibiting an IC50 of 10 μM. Research indicates that LY 78335 enhances spontaneous locomotor activity in rat models and elevates the extracellular concentration of 3-methoxy-4-hydroxyphenylglycol (MHPG) in the hypothalamus. Additionally, it has been shown to inhibit growth hormone secretion, making LY 78335 a valuable tool for studies related to depression and neuroendocrine function. -
Endogenous Metabolite
1-Hydroxypyrene serves as a primary endogenous metabolite and biomarker for exposure to polycyclic aromatic hydrocarbons (PAHs), particularly pyrenes. This compound is analyzed in urine samples to assess environmental and occupational exposure. Additionally, 1-Hydroxypyrene acts as an orally active agonist of the aryl hydrocarbon receptor (AhR), which is implicated in various biological processes, including renal fibrosis. Its significance in toxicological studies makes it a valuable reagent for research applications. -
LOX Inhibitor
SNT-5382 is a potent lysyl oxidase (LOX) inhibitor, designed to disrupt the enzymatic activity of LOX, which plays a critical role in extracellular matrix remodeling. This compound demonstrates significant biological activity in inhibiting tumor progression and metastasis, making it a valuable tool for cancer research. SNT-5382 can be utilized in various studies aimed at understanding the implications of LOX in malignancies and assessing potential therapeutic strategies. -
11β-HSD1 Inhibitor
11β-HSD1-IN-25 is a selective inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). This compound effectively reduces glucocorticoid levels both in vitro and in serum, while also diminishing lipid accumulation in various models. It modulates lipid metabolism through dual mechanisms involving the inhibition of 11β-HSD1 and activation of the AMP-activated protein kinase (AMPK) signaling pathway. 11β-HSD1-IN-25 is suitable for research applications focused on obesity and related metabolic disorders. -
DHFR Inhibitor
NSC309401 dihydrochloride is a selective inhibitor of dihydrofolate reductase (DHFR) from Escherichia coli, exhibiting an IC50 of 189 nM and a KD of 14.57 nM. This compound is primarily utilized in studies focused on microbial metabolism and antibiotic resistance. Its potent inhibition of DHFR makes it a valuable tool in researching folate biosynthesis pathways and developing novel therapeutic agents. -
Factor Xa Inhibitor
ChloraMine-T hydrate is a selective Factor Xa inhibitor known for its utility in synthetic chemistry. It serves as a versatile reagent in aminohydroxylation and allylic amination reactions, functioning as a nitrogen source in the aziridination of alkenes and facilitating the deprotection of sulfur groups in thiol-containing compounds. Additionally, ChloraMine-T hydrate exhibits antimicrobial properties, demonstrating efficacy against various bacterial strains, including Staphylococcus epidermidis, Staphylococcus aureus, Enterococcus faecalis, Escherichia coli, Proteus mirabilis, and Enterococcus cloacae, making it valuable for applications in both enzymatic inhibition studies and antimicrobial research. -
DGAT Inhibitor
1-Methyl-2-[(4Z,7Z)-4,7-tridecadienyl]-4(1H)-quinolone is a diacylglycerol acyltransferase (DGAT) inhibitor, demonstrating an IC50 of 20.1 μM. Additionally, it acts as an angiotensin II receptor blocker with an IC50 of 34.1 μM. This compound exhibits significant anti-Helicobacter pylori activity, with a minimum inhibitory concentration (MIC) of 10 μg/mL, making it valuable for studies investigating lipid metabolism and bacterial infections. -
Fungal Metabolite
BE 24566B is a polyketide fungal metabolite that acts as an endothelin receptor antagonist, targeting both ETA and ETB receptors with IC50 values of 11 μM and 3.9 μM, respectively. This compound demonstrates antibacterial activity against a range of Gram-positive bacteria, including B. subtilis, B. cereus, S. aureus, M. luteus, E. faecalis, and S. thermophilus, with reported MICs of 1.56 μg/mL for five of these species and 3.13 μg/mL for E. faecalis and S. thermophilus. BE 24566B is valuable for research applications in antimicrobial studies and receptor pharmacology. -
Cholecystokinin Receptor Antagonist
A-65186 is a cholecystokinin (CCK) A receptor antagonist that effectively inhibits CCK8-induced amylase secretion. This compound exhibits high binding affinity for pancreatic CCK-A receptors and demonstrates over 500-fold selectivity for CCK-A over CCK-B receptors. It serves as a valuable tool in research focused on gastrointestinal physiology and the role of CCK signaling in pancreatic function. -
CCK-A Receptor Agonist
A71378 is a selective CCK-A receptor agonist with an IC50 of 0.4 nM for the pancreatic CCK-A receptor, and significantly higher IC50 values for the cortical CCK-B and gastrin receptors at 300 nM and 1,200 nM, respectively. This compound effectively stimulates pancreatic amylase secretion with an EC50 of 0.16 nM and induces ileal muscle contraction with an EC50 of 3.7 nM. A71378 is valuable for research applications focusing on gastrointestinal pharmacology and the role of CCK-A receptors in digestive processes. -
CCK-4 Analog
A-70874 is a tyrosine-free tetrapeptide analog of cholecystokinin (CCK-4), acting as an agonist for pancreatic amylase release. It also serves as a partial agonist, promoting phosphoinositide decomposition in pancreatic cells. With an IC50 of 4.9 nM for the guinea pig pancreatic CCK receptor, A-70874 shows a notable affinity of 1.6 μM for the CCK-B/gastrin receptor. This compound is valuable for investigating the physiological roles of CCK receptors in both the digestive system and the central nervous system. -
Phospholipase D Inhibitor
Halopemide is a potent inhibitor of phospholipase D (PLD), exhibiting IC50 values of 220 nM for human PLD1 and 310 nM for PLD2. In addition to its enzymatic inhibition, Halopemide functions as a dopamine receptor antagonist and exhibits psychotropic properties. This reagent is valuable for research applications exploring PLD-mediated signaling pathways and dopamine receptor interactions in various biological contexts. -
PDE4B/D Inhibitor
PDE4B/D-IN-5 is a potent inhibitor of phosphodiesterase 4B and 4D, displaying IC50 values of 3.4 nM and 2.2 nM, respectively, with limited central nervous system penetration. This compound effectively inhibits TNF-α production and demonstrates significant anti-inflammatory, antioxidant, and anti-apoptotic properties by reducing the Bax/Bcl2 ratio and mitigating oxidative stress through decreased myeloperoxidase activity and nitric oxide levels. PDE4B/D-IN-5 is suitable for research applications in acute lung injury and related inflammatory conditions. -
Endogenous Metabolite
Hexadecanedioic acid, also known as Thapsic acid, is an endogenous metabolite that plays a crucial role in cellular metabolism. It inhibits IRE1α-mediated XBP1 splicing, thereby affecting flipogenesis and ferroptosis. Additionally, Hexadecanedioic acid downregulates the expression of XBP1 and Hrd1 while activating the Nrf2/SLC7A11/GPX4 pathway. This compound is valuable for research into metabolic-associated fatty liver disease and related metabolic disorders. -
MAO-B Inhibitor
Monoamine Oxidase B Inhibitor 6 is a highly selective, reversible, and competitive inhibitor of monoamine oxidase B (MAO-B) with a significant brain-blood barrier penetration capability, exhibiting an IC50 of 0.11 μM. This compound demonstrates notable antioxidant and neuroprotective properties and is applicable in the study of neurodegenerative diseases. Researchers investigating the role of MAO-B in neurobiology may find it a valuable tool for elucidating mechanisms of disease and exploring therapeutic avenues.
