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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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. -
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. -
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. -
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. -
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 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. -
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. -
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). -
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. -
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. -
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. -
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. -
CYP3A Inhibitor
ALT-2074 is a CYP3A inhibitor with an IC50 value ranging from 2.0 to 2.6 μM, functioning as a catalytic analogue of glutathione peroxidase. Although it demonstrates a weak inhibitory effect on CYP3A in vivo, it serves as a valuable tool for studying the role of oxidative stress in inflammatory diseases, including acute coronary syndrome. This compound is particularly useful in research investigating the interplay between reactive oxygen species and metabolic pathways. -
ALDH1A Inhibitor
ALDH1A Inhibitor 673A is a selective inhibitor targeting ALDH1A1, ALDH1A2, and ALDH1A3, with IC50 values of 246 nM, 230 nM, and 348 nM, respectively. This compound demonstrates minimal inhibitory effects on other ALDH family members. It has been shown to induce necroptotic death in ovarian cancer stem-like cells and cause DNA double strand breaks in cancer cells. ALDH1A Inhibitor 673A serves as a valuable tool for researching ovarian cancer mechanisms and treatment strategies. -
Necroptosis/11β-HSD1 Inhibitor
Necroptosis-IN-3 is a selective inhibitor of necroptosis, primarily targeting TNF-α induced necroptotic pathways. Additionally, this compound inhibits 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), thereby modulating glucocorticoid metabolism. Its key biological activities make it a valuable tool for researchers studying necroptosis and related cellular mechanisms in various disease models. -
Herbicide/Microtubule inhibitor
Ethalfluralin is a dinitroaniline herbicide that functions as a microtubule inhibitor. By disrupting intranuclear spindle formation, Ethalfluralin effectively obstructs nuclear division and cytokinesis in parasites. This compound also enhances phosphorylation of NF-κB and P38 MAPK while inhibiting the PI3K/AKT signaling pathway, leading to impaired mitochondrial functionality, apoptosis, endoplasmic reticulum stress, autophagy, and increased reactive oxygen species (ROS) production. Ethalfluralin is particularly relevant for research applications in toxoplasmosis and related parasitic diseases. -
DGAT-1 Inhibitor
Aphadilactone C is a selective inhibitor of diacylglycerol O-acyltransferase 1 (DGAT-1), exhibiting an IC50 of 0.46 μM. In addition to its DGAT-1 inhibition, Aphadilactone C demonstrates notable antimalarial properties with an IC50 value of 170 nM. This compound is valuable for research related to lipid metabolism and malaria treatment studies. -
PDEB1 Inhibitor
PDEB1-IN-1 is a selective inhibitor of Trypanosoma brucei phosphodiesterase B1 (TbrPDEB1), exhibiting an IC50 value of 0.95 μM. This compound effectively inhibits the proliferation of T. brucei, with an EC50 of 26 μM, making it a valuable tool for research in trypanosomiasis. PDEB1-IN-1 can be utilized in studies aimed at understanding the role of PDEB1 in the pathogenesis of the disease and for exploring therapeutic avenues in antiparasitic drug development. -
CYP51 Inhibitor
VNI is a potent inhibitor of cytochrome P450 51 (CYP51), targeting sterol synthesis in the parasite Trypanosoma cruzi. Its mechanism of action disrupts the biosynthesis of essential sterols, leading to impaired growth and viability of the pathogen. VNI is primarily utilized in research focused on anti-parasitic strategies and the development of therapeutics for Chagas disease. -
CYP51 Inhibitor
CYP51-IN-15 is a selective inhibitor of CYP51, targeting the enzyme in Naegleria fowleri. With an EC50 value of 1.5 μM, it demonstrates potent biological activity against this pathogenic organism. This compound is valuable in research aimed at elucidating mechanisms of action and developing therapeutic strategies against Naegleria fowleri infections. -
CYP51 Inhibitor
LP8 is a pyridinyl-type inhibitor of cytochrome P450 51 (CYP51), specifically targeting the sterol biosynthesis pathway in various pathogens. This compound exhibits significant biological activity against Trypanosoma cruzi, the causative agent of Chagas disease and American trypanosomiasis. LP8 is valuable for research applications aimed at elucidating the mechanisms of these diseases and developing potential therapeutic strategies. -
Pv NMT Inhibitor
NMT-IN-3 is a selective inhibitor of N-myristoyltransferase (NMT) targeting Plasmodium vivax. With an IC50 of 38 mM, it demonstrates significant inhibitory activity against Pv NMT. This reagent is valuable for studying myristoylation processes in malaria research and evaluating potential therapeutic strategies against Plasmodium infections. -
CYP3A Inhibitor
Cobicistat-d8 is a deuterated analog of Cobicistat, acting as a potent and selective inhibitor of cytochrome P450 3A (CYP3A) with IC50 values ranging from 30 to 285 nM. This reagent functions primarily as a pharmacokinetic enhancer, improving the absorption and bioavailability of anti-HIV agents. Its role in modulating drug metabolism makes it a valuable tool in pharmaceutical research and drug development. -
α-Glucosidase/HMG-CoA reductase Dual Inhibitor
Ganomycin I is a dual inhibitor targeting α-Glucosidase and HMG-CoA reductase. It demonstrates significant anti-diabetic properties and inhibits HIV protease, contributing to its potential as an antiviral agent. Additionally, Ganomycin I shows effectiveness in preventing osteoclastogenesis, making it a valuable reagent for research in diabetes and bone metabolism. -
α-Glucosidase I Inhibitor
Celgosivir hydrochloride is an α-glucosidase I inhibitor that demonstrates significant antiviral activity by inhibiting bovine viral diarrhoea virus (BVDV) with an IC50 value of 1.27 μM in in vitro assays. This compound is valuable for researchers studying viral infections and exploring potential therapeutic strategies through glycosidase inhibition. Its ability to modulate glycosylation processes makes it a relevant tool for biochemical and pharmacological investigations. -
Endoplasmic Reticulum α-glucosidase II (GluII) Inhibitor
ToP-DNJ is a specific inhibitor of endoplasmic reticulum α-glucosidase II (GluII), demonstrating an IC50 value of 9.0 μM. It selectively interferes with both catalytic reactions of GluII, showing enhanced activity in the initial conversion of di-glycosylated to mono-glycosylated glycans. Additionally, ToP-DNJ exhibits anti-DENV activity, making it a valuable tool for research into dengue virus infection and related glycobiology studies. -
Influenza Viru Inhibitor
SP187 hydrochloride is a host-targeting iminosaccharide that primarily inhibits endoplasmic reticulum glucosidase, rendering it effective against filovirus infections. This compound demonstrates antiviral activity, notably against the Dengue virus, in vivo. SP187 hydrochloride is a valuable tool for researchers investigating antiviral mechanisms and developing therapeutic strategies against viral infections. -
Glucosidase Inhibitor
Ganoderic acid Y is an α-glucosidase inhibitor, exhibiting an IC50 of 170 μM against yeast α-glucosidase. This compound demonstrates antiviral properties by inhibiting the replication of enterovirus 71 (EV71) through the disruption of the virus uncoating process. Ganoderic acid Y is relevant for research applications investigating glycosidase activity and antiviral strategies. -
Anti-oxidant, Lipid Peroxidation/5-lipoxygenase Inhibitor
LY221068 is a potent inhibitor of iron-dependent lipid peroxidation and 5-lipoxygenase, exhibiting notable antioxidant properties. This compound demonstrates significant anti-inflammatory activity, particularly in preclinical models of arthritis, such as the Freund's Complete Adjuvant-induced arthritis model in rats, where it effectively reduces bone damage and paw swelling. LY221068 serves as a valuable tool for investigating inflammatory processes and potential therapeutic approaches in arthritis research. -
MAO-A Inhibitor
Pirlindole mesylate is a selective and reversible inhibitor of monoamine oxidase A (MAO-A), playing a crucial role in the modulation of neurotransmitter metabolism. Additionally, Pirlindole exhibits antiviral activity against enterovirus D68 and coxsackievirus B3 (CV-B3), positioning it as a potential agent in virology research. This compound is valuable for studies focusing on depression, anxiety disorders, and the therapeutic mechanisms of neuronal regulation and viral infections. -
CYP1A1 Inhibitor
CYP1A1-IN-1 is a selective inhibitor of cytochrome P4501A1 (CYP1A1). This compound has demonstrated the ability to reduce bacterial loads of methicillin-resistant Staphylococcus aureus (MRSA) and Acinetobacter baumannii through the enhancement of macrophage phagocytosis. CYP1A1-IN-1 holds potential for advancing research in sepsis associated with multidrug-resistant (MDR) bacterial infections. -
DHFR Inhibitor
N-Didesmethyladitoprim is a metabolite of the selective bacterial dihydrofolate reductase (DHFR) inhibitor, Aditoprime. This compound effectively inhibits the conversion of dihydrofolic acid to tetrahydrofolic acid, demonstrating an IC50 of 47 nM against E. coli and 520 nM against L. casei DHFR. N-Didesmethyladitoprim exhibits broad-spectrum antibacterial activity and possesses favorable pharmacokinetic properties, making it a valuable tool for research in antimicrobial mechanisms and DHFR inhibition studies. -
DHFR Inhibitor
NSC309401 is a potent inhibitor of dihydrofolate reductase (DHFR) from E. coli, exhibiting an IC50 value of 189 nM and a KD of 14.57 nM. This compound is essential for studying folate metabolism and can be utilized in research applications related to antimicrobial drug development and cancer therapeutics. Its specificity for DHFR makes it a valuable tool for elucidating the biochemical pathways influenced by folate synthesis. -
DHFR Inhibitor
DHFR-IN-10 is a potent inhibitor of dihydrofolate reductase (DHFR), exhibiting an IC50 of 4.21 μM against M. tuberculosis DHFR. This compound demonstrates significant antituberculosis efficacy, making it a valuable tool in research focused on combating tuberculosis and studying DHFR-related pathways. Its effectiveness positions DHFR-IN-10 as a potential lead candidate for further development in anti-tubercular drug discovery.
