-
DHFR Inhibitor
DDPO is a potent inhibitor of dihydrofolate reductase (DHFR) with an IC50 of 0.035 µM. This compound demonstrates significant anticancer activity by inhibiting the growth of L1210 and WI-L2 cell lines, with IC50 values of 5 µM and 0.28 µM, respectively. DDPO is primarily used in research applications focusing on cancer therapeutics and DHFR-related pathways. -
Endogenous Metabolite
DL-Norvaline is a derivative of L-norvaline that serves as a non-competitive inhibitor of arginase. By inhibiting this enzyme, DL-Norvaline can influence the L-arginine metabolism pathway, affecting nitric oxide production and supporting various biological processes. It is utilized in research applications focused on metabolic pathways, nitric oxide synthesis, and related physiological effects. -
DHFR/TS Inhibitor
CB 3705 is a potent inhibitor of dihydrofolate reductase (DHFR) and thymidylate synthetase (TS). This compound demonstrates significant anti-cancer activity, exhibiting ID50 values of 4.77 μM against L1210 cells and 408 μM against the mutant L1210:C15 cell line. Its inhibition of key enzymes involved in nucleotide synthesis makes CB 3705 a valuable tool for cancer research and drug development. -
AhR Agonist
MeBIO is a potent aryl hydrocarbon receptor (AhR) agonist, exhibiting an IC50 of 44 μM for GSK-3 and 55 μM for CDK1/cyclin B interactions. This compound is primarily utilized in research to explore the role of AhR signaling in various biological processes, such as immune response regulation and cellular differentiation. Researchers can employ MeBIO to investigate its effects in toxicology studies and the development of therapeutic strategies targeting AhR pathways. -
GSK3β Inhibitor
GSK3β-IN-3 is an ATP-competitive inhibitor of glycogen synthase kinase 3 beta (GSK3β), exhibiting an IC50 of 0.90 μM. It effectively lowers the phosphorylation levels of tau protein in the BR5706 strain and reduces the accumulation of amyloid-beta (Aβ) aggregates in the CL2006 strain. This compound is essential for research applications focused on Alzheimer's disease (AD), aiding in the understanding of neurodegenerative mechanisms and potential therapeutic strategies. -
Endogenous Metabolite
Farnesol is a sesquiterpene alcohol that functions as an endogenous metabolite with notable antimicrobial properties. It has been shown to modulate cell-to-cell communication in Candida albicans and exhibits inhibitory activity against various bacterial species. This compound is valuable for research in microbial interactions and the modulation of pathogenic behaviors. -
α-glucosidase Inhibitor
1-Deoxynojirimycin hydrochloride is a potent α-glucosidase inhibitor, primarily utilized for modulating postprandial blood glucose levels. This compound demonstrates notable antihyperglycemic and anti-obesity effects, making it valuable in diabetes mellitus research. Additionally, 1-Deoxynojirimycin hydrochloride exhibits antiviral properties, contributing to its diverse applicability in metabolic and infectious disease studies. -
HMG-CoA Synthase Inhibitor
Hymeglusin is a fungal β-lactone antibiotic that functions as a potent inhibitor of HMG-CoA synthase, exhibiting an IC50 of 0.12 μM. This compound covalently modifies the active cysteine residue at position 129 of the enzyme, thereby disrupting its activity. Hymeglusin is primarily utilized in research applications focused on lipid metabolism and studying the modulation of cholesterol biosynthesis pathways. -
Phospholipase C Inhibitor, Angiogenesis Modulator
Neomycin is an aminoglycoside antibiotic known for its role as a phospholipase C (PLC) inhibitor and angiogenesis modulator. It effectively inhibits the nuclear translocation of angiogenin, resulting in reduced cell proliferation and angiogenesis. Additionally, Neomycin interferes with IP3-mediated calcium release and MgATP-dependent calcium uptake, influencing skeletal muscle calcium transients. Its ability to modulate crucial biological pathways makes Neomycin a valuable tool for cancer research and understanding microbial impact on health. Prolonged exposure may lead to adverse effects such as hearing impairment and kidney damage. -
MAO-A/B Inhibitor
Tedizolid phosphate sodium is a selective inhibitor of monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B). This compound exhibits significant activity against Gram-positive bacteria, making it valuable in the study of antimicrobial resistance and the development of new therapeutic agents. Its mechanisms of action and inhibition properties facilitate research into neurological disorders and other conditions associated with monoamine dysregulation. -
Cytochrome P450 Inhibitor
Kushenol K is a flavonoid antioxidant derived from the roots of Sophora flavescens, functioning as a selective inhibitor of cytochrome P450 3A4 (CYP3A4) with a Ki value of 1.35 μM. This compound exhibits weak antiviral activity against herpes simplex virus type 2 (HSV-2) with an EC50 of 147 μM. Additionally, Kushenol K inhibits sodium-glucose co-transporters SGLT1 and SGLT2, making it relevant for research in metabolic disorders and viral infections. -
Fungal Metabolite
Colletodiol is a fungal metabolite that demonstrates immunosuppressant and antiviral activities. This compound effectively inhibits concanavalin A- or LPS-induced proliferation of isolated mouse splenocytes, with IC50 values of 12 and 5 μg/mL, respectively. Additionally, Colletodiol has been shown to inhibit influenza A viral replication in HeLa-IAV-Luc cells, making it a valuable tool for research in immunology and virology. -
MAO Inhibitor
Eckol is a potent inhibitor of human monoamine oxidase A (hMAO-A) and a non-competitive inhibitor of human monoamine oxidase B (hMAO-B), with IC50 values of 7.20 μM and 83.44 μM, respectively. This compound exhibits significant biological activity through its antiallergic and antiviral effects, making it a valuable tool for exploring these pathways. Additionally, Eckol promotes stimulatory effects in maize and may serve as an effective plant biostimulant in agricultural research applications. -
CYP51 Inhibitor
Obtusifoliol is a selective inhibitor of cytochrome P450 51 (CYP51), demonstrating affinities with dissociation constants (Kd) of 1.2 μM for Trypanosoma brucei and 1.4 μM for human CYP51. This compound is significant in studies focused on trypanosomiasis, targeting the sterol biosynthesis pathway. Its inhibition of CYP51 may provide valuable insights into therapeutic strategies against related infections and contribute to the understanding of cholesterol metabolism in various biological systems. -
ChE Inhibitor
N-p-trans-Coumaroyltyramine is a natural phenolic amide compound that acts as an inhibitor of acetylcholinesterase (AChE) with an IC50 of 122 μM and α-glucosidase with an IC50 of 2.7 μM. It demonstrates significant anti-trypanosomal activity, exhibiting an IC50 of 13.3 µM against Trypanosoma brucei rhodesiense. This compound is valuable for research into neurodegenerative diseases such as Alzheimer's disease, as well as for studies focusing on trypanosomiasis. -
Endogenous Metabolite
L-Canaline is a nonprotein amino acid primarily associated with leguminous plants. It acts as a potent and irreversible inhibitor of ornithine aminotransferase and exhibits cytotoxic properties. L-Canaline has demonstrated significant antiproliferative effects and inhibits the growth of the malaria parasite Plasmodium falciparum, with an IC50 value of 297 nM. This compound is valuable for research applications in cancer biology and metabolic studies involving endogenous metabolites. -
Endogenous Metabolite
Tridecanedioic acid is an endogenous metabolite that plays a significant role in metabolic regulation, particularly in the context of non-alcoholic fatty liver disease (NASH). This compound serves as a potential node in the interaction network between intestinal microbiota and host metabolism. It is notably accumulated in resilient cabbage-type rapeseed varieties, indicating its involvement in plant defense mechanisms against pests such as the small cabbage moth (Plutella xylostella). Additionally, tridecanedioic acid may serve as a valuable biomarker for assessing plant insect resistance and diagnosing metabolic diseases. -
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. -
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.

