Catalog No.
Product Name
Application
Product Information
Citations
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AChE/BACE1/GSK3β Inhibitor
AChE/BACE1/GSK3β-IN-1 is a potent triple inhibitor targeting acetylcholinesterase (AChE), beta-secretase 1 (BACE1), and glycogen synthase kinase 3 beta (GSK3β). It demonstrates effective inhibitory activity with IC50 values of 1.0 μM for AChE, 20 μM for BACE1, and 15 μM for GSK3β. With favorable blood-brain barrier penetrability and bioavailability, AChE/BACE1/GSK3β-IN-1 is a valuable tool for research into Alzheimer's disease mechanisms and therapeutics. -
AChE/GSK-3β Inhibitor
ZLWH-23 is a selective inhibitor of acetylcholinesterase (AChE) with an IC50 of 0.27 μM and also inhibits glycogen synthase kinase-3 beta (GSK-3β) with an IC50 of 6.78 μM. It exhibits greater selectivity for AChE compared to butyrylcholinesterase (BChE) and shows preferential inhibition of GSK-3β over a range of multi-kinases. This compound is relevant for research focused on Alzheimer's disease pathophysiology. -
AChE/GSK-3β Inhibitor
PJ17 is a potent dual inhibitor of acetylcholinesterase (AChE) and glycogen synthase kinase 3 beta (GSK-3β), exhibiting IC50 values of 8.84 μM and 4.19 μM, respectively. This compound demonstrates a lack of significant neurotoxicity in primary cerebellar granule neuron cultures, making it a promising candidate for neuropharmacological studies. PJ17 serves as a valuable template for the development of multitarget therapeutics and is relevant in research focused on Alzheimer's disease. -
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. -
hAChE/hBuChE Inhibitor
hAChE-IN-5 is a potent inhibitor of human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBuChE), exhibiting IC50 values of 0.17 μM for both enzymes. In addition, hAChE-IN-5 demonstrates significant GSK3β inhibition with an IC50 of 0.21 μM. This compound is utilized in research focused on tau protein aggregation and Aβ1-42 self-aggregation, effectively preventing Aβ-dependent neurotoxicity. Furthermore, hAChE-IN-5 can cross the blood-brain barrier, showcasing its potential as a multi-targeted agent in the study of Alzheimer's disease. -
5-LO/COX-2/DPP-4 Inhibitor
Timosaponin A1 is a natural steroidal saponin that acts as an inhibitor of 5-lipoxygenase (5-LO), cyclooxygenase-2 (COX-2), and dipeptidyl peptidase 4 (DPP-4), with IC50 values of 3.29 µM, 36.43 µM, and 33.25 µM, respectively. This compound exhibits anti-inflammatory properties and is relevant for research on conditions such as asthma and diabetes. Its inhibitory effects on key enzymes involved in inflammatory pathways make it a valuable tool for exploring therapeutic strategies in related biological studies. -
ACE Inhibitor
Ovotransferrin (328-332) is an Angiotensin-Converting Enzyme (ACE) inhibitor that demonstrates protective effects on blood pressure, with an IC50 of 20 μM. Additionally, this fragment exhibits activity against Cholinesterase (ChE), highlighting its potential relevance in Alzheimer's disease research. Its dual inhibitory mechanisms make it a valuable tool for studying cardiovascular health and neurodegenerative disorders. -
Antibacterial Agent
Tellimagrandin II is an antibacterial agent that disrupts the integrity of the cell wall in Staphylococcus aureus, leading to cell lysis and loss of cytoplasmic contents. Additionally, it demonstrates anti-inflammatory properties and inhibits acetylcholinesterase (AChE), which may contribute to improvements in memory impairment. This compound is of interest in research focusing on antibacterial strategies, inflammatory pathways, and neurodegenerative conditions. -
Antibiotic
Manumycin B is an antibiotic that also demonstrates notable antitumor activity. It functions as an inhibitor of acetylcholinesterase (AChE), exhibiting an IC50 value of 15 mM. This compound is valuable for research in cancer biology and neuropharmacology, providing insights into therapeutic strategies for cancer treatment and neurodegenerative disorders. -
nAChR Agonist
Pyrantel is an orally active anthelmintic that functions as an agonist of the nicotinic acetylcholine receptor (nAChR). It induces spasmodic muscle paralysis in parasitic organisms, making it effective in the eradication of a variety of helminthic infections. Pyrantel is commonly utilized in the study and treatment of conditions such as ascariasis, hookworm infections, pinworm infections, and trichinosis, providing critical research insights into parasitic diseases. -
AAK1 Inhibitor
SGC-AAK1-1 is a potent and selective inhibitor of AP2 associated kinase 1 (AAK1), exhibiting an IC50 of 270 nM and a Ki of 9 nM. In addition to its primary target, SGC-AAK1-1 also strongly inhibits BMP2K. This compound is valuable for research into the Wnt signaling pathway, particularly in studies related to the function and regulation of AAK1. -
COX-2 Inhibitor
APHS is a selective and covalent inhibitor of cyclooxygenase-2 (COX-2) that exerts neuroprotective effects. By acetylating serine 516 in the active site of COX-2, APHS effectively inhibits prostaglandin production, which is often upregulated in colorectal cancer. In addition to its role as a COX-2 inhibitor, APHS also co-inhibits the WNT signaling pathway, contributing to its anti-tumor mechanisms. This compound is valuable for research into cancer biology and neuroprotection. -
COX-2 Inhibitor
Thymohydroquinone is a selective inhibitor of cyclooxygenase-2 (COX-2) with noted anti-SARS-CoV-2 activity. It exhibits cytotoxic properties, antiproliferative effects, and the ability to suppress tumor growth in various cancer models. This compound is applicable in research focused on squamous cell carcinoma, fibrosarcoma, and the pathogenesis and treatment of COVID-19 caused by SARS-CoV-2. -
nAChR Aagonist
Simpinicline (OC-02) is a highly selective agonist of the nicotinic acetylcholine receptor (nAChR). This compound exhibits potent antiviral activity against SARS-CoV-2 variants in cell culture, with an IC50 value of 0.04 µM. Its unique selectivity and efficacy make it a valuable tool for research in virology and neuropharmacology. -
Natural Compound
Lucidadiol is a natural compound derived from Ganoderma lucidum, functioning as an acetylcholinesterase inhibitor with an IC50 value of 31 μM. This compound also demonstrates antiviral activity against influenza virus type A and herpes simplex virus type 1 (HSV-1). Lucidadiol is valuable for research applications exploring neuroprotective mechanisms and viral infection inhibition. -
Anthelmintic Agent/Immunoregulatory Agent
Levamisole is an anthelmintic agent recognized for its immunoregulatory properties. This compound functions as a positive allosteric modulator of the α3β2 (EC50 = 300 μM) and α3β4 (EC50 = 100 μM) subtypes of nicotinic acetylcholine receptors (nAChRs), enhancing receptor activity. It is orally active and is commonly used in research applications related to parasitic infections and immune response modulation. -
AChE Inhibitor
Coumaran, also known as 2,3-Dihydrobenzofuran, is an inhibitor of acetylcholinesterase (AChE) and exhibits notable antileishmanial activity. Its mechanisms include the activation of macrophages, contributing to its antiparasitic effects and immunomodulatory properties. Coumaran is also applicable in the field of biopesticides, providing a potential tool for agricultural and biological research. -
Nicotinic acetylcholine receptors Inhibitor
Dinotefuran is a competitive inhibitor targeting insect nicotinic acetylcholine receptors (nAChRs). This compound effectively disrupts neural signaling in insects, leading to dysfunction. With an IC50 of 890 nM for [3H]epibatidine and 36.1 μM for [3H]α-bungarotoxin in American cockroach neural membranes, Dinotefuran demonstrates significant knockdown (KD50=0.351 nmol/g) and lethal activity (LD50=0.173 nmol/g) against German cockroach. Its primary applications include agricultural pest control, specifically targeting piercing-sucking and chewing insects like aphids and planthoppers, and it also serves as a tool for studying environmental toxicological impacts such as oxidative stress and reproductive neurotoxicity in earthworms. -
Glucosylceramide Synthase Inhibitor
DL-threo-PDMP hydrochloride is a competitive inhibitor of glucosylceramide synthase (GCS), demonstrating significant potential in antimalarial research. This compound effectively inhibits GCS activity, leading to restored sensitivity to cisplatin in cisplatin-resistant testicular germ cell tumor cells. Additionally, DL-threo-PDMP hydrochloride has been shown to impede the growth of ring-stage Plasmodium falciparum parasites, making it a valuable tool for studying malaria and its treatment. -
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. -
Parasite Inhibitor
Diazinon is an irreversible acetylcholinesterase (AChE) inhibitor with primary applications in pest control as an insecticide. By inhibiting AChE, Diazinon leads to the accumulation of acetylcholine, resulting in overstimulation of acetylcholine receptors and disruption of nervous system function. Additionally, Diazinon generates reactive oxygen species (ROS), contributing to oxidative stress across various biological tissues. This compound is predominantly utilized in agricultural settings but may also hold implications for human and animal health research. -
AChE Inhibitor
Carbosulfan is an orally active acetylcholinesterase (AChE) inhibitor that hydrolyzes to carbofuran, leading to significant insecticidal properties. This compound demonstrates broad-spectrum insecticidal activity while inducing oxidative stress through increases in lipid peroxidation and impairment of antioxidant defenses. Carbosulfan is associated with reproductive toxicity in male rats and developmental disorders in offspring, making it a relevant subject in studies focused on reproductive toxicity and environmental risk assessment. Its persistence in aquatic environments raises concerns regarding potential hazards to non-target organisms. -
Parasite Inhibitor
8-Deoxygartanin, a prenylated xanthone derived from Garcinia mangostana, serves as a selective inhibitor of butyrylcholinesterase (BChE). This compound demonstrates significant antiplasmodial activity, with an IC50 value of 11.8 μM against the W2 strain of Plasmodium falciparum. Additionally, 8-Deoxygartanin inhibits NF-κB (p65) activation, displaying an IC50 of 11.3 μM, making it a valuable reagent for research in parasitic infections and inflammation pathways. -
Organophosphorus Insecticide
Pirimiphos-methyl is an organophosphorus insecticide and acaricide that acts as an acetylcholinesterase (AChE) inhibitor in target organisms. This compound is effective in the prevention and control of a variety of pests, including beetles, snout beetles, moths, and Ephestia cautella, particularly during the storage of agricultural grains. Its efficacy in disrupting neural signaling makes it valuable for research into pest management strategies and environmental impact studies in agricultural settings. -
nAChR Antagonist
Derquantel is a spirocyclic anthelmintic that functions as a competitive antagonist of nicotinic acetylcholine receptors (nAChRs). It inhibits acetylcholine-induced depolarization with an IC50 of 0.22 μM, leading to flaccid paralysis of nematode somatic muscles. This mechanism effectively dislodges parasites from the host gastrointestinal tract, making Derquantel a valuable tool in research related to Haemonchus contortus and Ascaris suum infections. -
Cholinesterase (ChE) Inhibitor
Fenchlorphos is an organophosphate compound that acts as a potent inhibitor of acetylcholinesterase (AChE), an important enzyme in cholinergic signaling. By disrupting AChE activity, Fenchlorphos leads to the accumulation of acetylcholine, resulting in increased cholinergic neurotransmission. Additionally, this compound has been shown to induce mitochondrial dysfunction, making it a valuable tool for research on neurobiology and toxicology. Its applications include studies on the mechanisms of insecticide action and investigations into the impacts of cholinergic inhibition on cellular metabolism. -
Carbamate Insecticide
Pirimicarb is a selective carbamate insecticide that functions as an acetylcholinesterase (AChE) inhibitor, making it effective against a variety of pests. It exhibits rapid action and is suitable for use on a broad spectrum of crops, including cereals, sugar beet, potatoes, fruits, and vegetables. Pirimicarb's efficacy extends to its acaricidal properties, supporting extensive research in agricultural pest control mechanisms. -
Parasite
Triazophos is a potent non-systemic insecticide and acaricide that functions as an acetylcholinesterase (AChE) inhibitor. By covalently and irreversibly binding to the acetylcholine binding site, Triazophos effectively disrupts the hydrolysis of acetylcholine, resulting in increased neuroexcitability. This compound demonstrates efficacy against a broad spectrum of soil insects and mites, including aphids, thrips, and spider mites, making it valuable for crop protection in various agricultural settings, such as ornamentals, cotton, rice, maize, soybeans, oil palms, olives, and coffee. -
Parasite Inhibitor
Phosalone is an organophosphate insecticide that primarily targets acetylcholinesterase, leading to the inhibition of neurotransmission in parasites. Its potent biological activity makes it effective in controlling a wide range of insect pests. Phosalone is utilized in entomological research and in studies focusing on pest management strategies and the biochemical pathways of insecticide resistance. -
nAChR Modulator
GSK575594A is an allosteric modulator of the nicotinic acetylcholine receptor (nAChR) in Ascaris suum. This compound enhances muscle contractions triggered by acetylcholine (ACh) by binding to the allosteric site within the transmembrane domain of the nAChR, leading to a significant increase in contraction amplitude (Emax from 1.19 g to 1.51 g) at a concentration of 3 μM. GSK575594A is applicable in antiparasitic research, providing insights into neuromuscular mechanisms in parasitic infections. -
ChE Inhibitor
Isogarcinol is a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), exhibiting IC50 values of 1.13 μM and 8.30 μM, respectively. This compound also demonstrates significant leishmanicidal activity, with an IC50 of 0.33 μM against Leishmania donovani. Isogarcinol's dual action makes it a valuable tool for research in neurodegenerative disorders and parasitic diseases. -
Stable Isotope
Temephos-d12 is a deuterated form of Temephos, an organophosphate larvicide. It targets the central nervous system of aquatic larvae, including those of mosquitoes, midges, and black flies, by inhibiting cholinesterase activity. This mechanism leads to larval mortality prior to reaching the adult stage, making Temephos-d12 valuable for research on pesticide efficacy and environmental impact studies. -
Stable Isotope
(R)-3-O-Methyldopa-d3 is a deuterated form of the R-enantiomer of 3-O-Methyldopa, which acts as a metabolite of L-DOPA. The compound exerts its biological activity by competitively inhibiting catechol-O-methyltransferase (COMT), thus influencing the pharmacological effects of both L-DOPA and dopamine. This stable isotope is essential for research applications involving metabolic pathways and neurological studies. -
Anti-aggregation Agent
CLR01 sodium is an anti-aggregation agent that effectively penetrates the blood-brain barrier. It inhibits the de novo aggregation of key proteins, including Amyloid-β 40/42, α-synuclein, IAPP, tau protein, and SOD1. CLR01 sodium has demonstrated the ability to reduce amyloid plaque burden in the cortex of triple-transgenic mice, resulting in improvements in memory and motor functions. This compound is applicable in research focused on neurodegenerative disorders such as Alzheimer's disease, Parkinson's disease, and amyotrophic lateral sclerosis (ALS). -
P2Y1 receptor/[35S]GTPγS binding/β-arrestin 2 recruitment Agonist
MRS2365 is a highly potent and selective agonist of the P2Y1 receptor, exhibiting an EC50 of 0.4 nM for [35S]GTPγS binding and β-arrestin 2 recruitment. This compound effectively alleviates mechanical allodynia and enhances mechanical sensitivity, making it valuable for pain research. Notably, MRS2365 demonstrates minimal activity at P2Y12 and P2Y13 receptors, highlighting its specificity for P2Y1. -
BChE Inhibitor/CB2R Agonist
hBChE-IN-2 is a potent butyrylcholinesterase (BChE) inhibitor with an IC50 of 0.62 μM and functions as an agonist for cannabinoid receptor 2 (CB2R). This compound exhibits significant neuroprotective activities, making it a valuable tool in the study of neurodegenerative diseases and cannabinoid signaling pathways. Its dual action positions hBChE-IN-2 as an important reagent for research applications targeting cholinergic regulation and endocannabinoid modulation. -
Topoisomerase I Inhibitor
RPR121056 is a topoisomerase I inhibitor that functions as a metabolite of the chemotherapy agent Irinotecan (CPT-11), produced by the enzyme CYP3A4. This compound induces cell death by disrupting DNA replication, making it relevant for cancer research, particularly in the context of colorectal cancer treatment. Additionally, RPR121056 demonstrates direct inhibition of acetylcholinesterase (AChE), further expanding its potential applications in pharmacological studies. -
Stable Isotope
RPR121056-d3 is a deuterated analog of RPR121056, a metabolite of the anticancer drug Irinotecan. It primarily targets and inhibits topoisomerase type I, leading to apoptosis in cancer cells. RPR121056-d3 is utilized in research applications focused on understanding the metabolic pathways and pharmacokinetics of Irinotecan, particularly in the context of colorectal cancer therapy. Additionally, it may also provide insights into the inhibition of acetylcholinesterase (AChE). -
Alkaloid
Aposcopolamine is an alkaloid isolated from Datura ferox, known for its ability to bind closely with acetylcholinesterase (ACHE), adrenergic receptor alpha-2A (ADRA2A), and muscarinic receptor subtype 2 (CHRM2). This compound is of significant interest in Alzheimer's disease research due to its potential effects on cholinergic signaling pathways. Aposcopolamine serves as a valuable tool in investigating neurodegenerative mechanisms and developing therapeutic strategies. -
M3 mAChR Antagonist
p-F-HHSiD hydrochloride is a potent and selective antagonist of the M3 muscarinic acetylcholine receptor (mAChR). This compound also demonstrates antagonistic properties towards other mAChR subtypes and the alpha1-adrenoceptor. p-F-HHSiD hydrochloride is useful for research applications involving cancer, metabolic disorders, neurological conditions, and cardiovascular diseases, including colon cancer, Alzheimer’s disease, and diabetes. -
mAChR Antagonist
Batefenterol Succinate is an inhaled bifunctional bronchodilator that acts as a muscarinic acetylcholine receptor (mAChR) antagonist and a beta2-adrenoceptor agonist. This dual mechanism results in effective smooth muscle relaxation, enhancing respiratory function. Batefenterol Succinate is primarily utilized in research focused on chronic obstructive pulmonary disease (COPD) and other respiratory conditions, providing insights into therapeutic strategies for airway obstruction. -
mAChR/Adrenergic Receptor Antagonist
Muscarinic toxin 3 (MT3) is a selective and non-competitive antagonist of muscarinic acetylcholine receptors (mAChRs) and adrenergic receptors. It exhibits high potency with pIC50 values of 6.71, 8.79, 8.86, 7.57, 8.13, and 8.49 against M1, M4, α1A, α1B, α1D, α2A, α2B, and α2C receptors, respectively, highlighting its prominent adrenoceptor activity. This compound is valuable in studying receptor signaling pathways and has potential applications in pharmacological research focused on nervous system disorders and cardiovascular diseases. -
M3 mAChR Antagonist
p-F-HHSiD (p-Fluorohexahydrosiladifenidol) functions as a selective antagonist of the M3 muscarinic acetylcholine receptor (mAChR). This compound exhibits antagonistic activity against various muscarinic receptor subtypes as well as the alpha-1 adrenergic receptor. p-F-HHSiD is valuable for research in cancer, metabolic disorders, neurological pathologies, and cardiovascular diseases, including colon cancer, Alzheimer's disease, and diabetes. -
P2Y14R Antagonist
MK-852 is a potent P2Y14 receptor antagonist that plays a crucial role in modulating platelet aggregation. This compound effectively inhibits the binding of fibrinogen to platelets in vitro, making it a valuable tool for studying thrombotic processes. Research applications include investigations into platelet function and the development of antithrombotic therapies. -
Babesicidal Agent
Quinuronium disulfate is a potent babesicidal agent with demonstrated anticholinesterase activity. It is primarily utilized in the study of protozoan infections, particularly those caused by Babesia species. This compound serves as a valuable tool in researching therapeutic interventions for babesiosis and related parasitic diseases. -
AChE/Dopamine 2 Inhibitor
Itopride is a potent dopamine D2 receptor antagonist and an acetylcholinesterase (AChE) inhibitor. Itopride enhances gastric motility through its dual mechanisms of action, promoting both antidopaminergic and anti-acetylcholinesterase effects. This compound is primarily utilized in research related to gastrointestinal disorders, particularly gastroesophageal reflux disease (GERD), offering insights into prokinetic therapies. -
Anti-tumor Agent
Scoulerine hydrochloride is a multi-target inhibitor primarily acting as an anti-tumor agent. It disrupts the PI3K/Akt/mTOR signaling pathway and α1D-adrenergic receptors, leading to microtubule destabilization, cell cycle arrest, and apoptosis in cancer cells. This compound also inhibits mitochondrial dehydrogenase activity and demonstrates effects on GABA receptors and BACE1, suppressing tumor cell proliferation, migration, invasion, and stem cell-like properties. Additionally, Scoulerine hydrochloride exhibits pharmacological activities against Plasmodium falciparum, as well as antibacterial, antiemetic, and antitussive properties, while also influencing endoplasmic reticulum stress and mitochondrial function. It is particularly relevant in studies focused on leukemia, ovarian cancer, and colorectal cancer. -
Insecticide
Chlorphoxim is a highly efficient insecticide that acts by inhibiting acetylcholinesterase (AChE), leading to the disruption of neurotransmission in target pests. This compound also demonstrates the ability to inhibit superoxide dismutase (SOD) and catalase (CAT) activities in zebrafish embryos, thereby inducing oxidative stress through the activation of reactive oxygen species (ROS). Additionally, Chlorphoxim promotes apoptosis in zebrafish embryos by modulating the expression of pro-apoptotic and anti-apoptotic proteins such as Bax, Bcl2, and p53. Its neurotoxic and developmental effects make Chlorphoxim a key compound for agricultural research aimed at pest control. -
COX-1 Inhibitor
NCX 466 is a selective inhibitor of COX-1 and COX-2, demonstrating notable anti-inflammatory and analgesic properties. It functions as a nitric oxide (NO) donor, enhancing microcirculation while exerting antioxidant effects. NCX 466 effectively reduces levels of transforming growth factor-β (TGF-β) and oxidative stress markers, including thiobarbituric acid reactive substances (TBARS) and 8-hydroxy-2'-deoxyguanosine (8-OHdG). Furthermore, it mitigates leukocyte recruitment during inflammatory responses by decreasing myeloperoxidase (MPO) activity, contributing to the prevention of bleomycin-induced pulmonary fibrosis in murine models. -
P2Y14R Antagonist
HDL-16 is a highly potent antagonist of the P2Y14 receptor, exhibiting an IC50 of 0.3095 nM. This compound demonstrates significant biological activity by alleviating dextran sulfate sodium (DSS)-induced colitis, primarily through the inhibition of necroptosis in intestinal epithelial cells (IECs) and the preservation of mucosal barrier function. HDL-16 is valuable for research applications focused on inflammatory bowel diseases and related gastrointestinal disorders.
