AChE

Cat. No.

A30276

CAS No.

23740-25-2

Lanuginosine

Lanuginosine is an alkaloid with demonstrated anticancer activity. It induces apoptosis and inhibits acetylcholinesterase (AChE) with an IC50 of 10.9 μM, in addition to preventing amyloid-beta (Aβ) aggregation. This compound exhibits potent anticancer effects against various malignancies, including hepatocellular carcinoma, human promyelocytic leukemia, chronic myeloid leukemia, melanoma, and brain tumors. Lanuginosine is also valuable for research related to Alzheimer's disease and its therapeutic strategies.

Cat. No.

A30479

CAS No.

60-51-5

Dimethoate

Dimethoate is an organophosphate insecticide and acaricide that functions primarily as an acetylcholinesterase inhibitor. It exhibits significant biological activity by inducing reactive oxygen species (ROS) production, leading to DNA damage and apoptosis in vivo. Additionally, Dimethoate impacts the immune system in murine models, highlighting its relevance in toxicological and environmental research applications.

Cat. No.

A30836

CAS No.

31059-54-8

β-NETA

β-NETA is a potent noncompetitive inhibitor of cholinesterase (ChE) and choline acetyltransferase (ChA), with IC50 values of 40 μM and 76 μM, respectively. Additionally, it exhibits weak inhibitory effects on acetylcholinesterase (AChE), with an IC50 value of 1 mM. This compound is relevant for research in neurobiology and studies focused on cholinergic signaling pathways and associated disorders.

Cat. No.

A30840

CAS No.

639-14-5

Gypsogenin

Gypsogenin is a selective mixed-type inhibitor of butyrylcholinesterase (BChE) with a Ki of 19.99 μM. It demonstrates significant cytotoxicity against multiple human cancer cell lines by inducing cell cycle arrest and initiating apoptosis. Additionally, Gypsogenin exhibits antibacterial properties against species such as Bacillus subtilis and Bacillus thuringiensis, positioning it as a crucial scaffold for developing novel anticancer agents. This compound is extensively utilized in research focusing on Alzheimer's disease and various cancers, including colon cancer, melanoma, and leukemia.

Cat. No.

A30941

CAS No.

1219794-81-6

Dimethoate-d6

Dimethoate-d6 is a deuterium-labeled analogue of Dimethoate, an organophosphate insecticide and acaricide. It functions primarily as an acetylcholinesterase inhibitor, leading to enhanced neurotransmitter activity. This compound demonstrates significant biological activities, including the induction of reactive oxygen species (ROS), DNA damage, and cell apoptosis in vivo. Additionally, Dimethoate-d6 has been shown to affect immune system responses in murine models, making it a valuable tool for research in toxicology and environmental sciences.

Cat. No.

A31086

CAS No.

1128109-00-1

Galanthamine-d6

Galanthamine-d6 is a deuterium-labeled derivative of Galanthamine, a potent inhibitor of acetylcholinesterase (AChE) with an IC50 value of 500 nM. This stable isotope compound is valuable in pharmacokinetic studies and metabolic research, particularly in exploring the mechanisms of cholinergic modulation. Its isotopic labeling helps in the precise tracking of metabolite pathways in biological assays.

Cat. No.

A31087

CAS No.

501-26-8

Cardanol monoene

Synonyms: Cardanol C15:1

Cardanol monoene is a phenolic compound derived from cashew nut shell liquid, primarily targeting cellular mechanisms involved in cancer progression. It exhibits significant anti-cancer activities, including the inhibition of cell proliferation and migration, S phase arrest, and induction of apoptosis via reactive oxygen species (ROS) production and mitochondrial depolarization. Cardanol monoene modulates key signaling pathways by downregulating MMP-2 and MMP-9 expressions and regulating the expression of CDK2, p53, and Bax, among others. Additionally, it demonstrates weak DPPH radical scavenging and acetylcholinesterase inhibition activities, making it suitable for research in cancer, infection, and inflammation.

Cat. No.

A31355

CAS No.

484-08-2

Kokusaginine

Kokusaginine is a furoquinoline alkaloid that acts as an acetylcholinesterase (AChE) inhibitor, exhibiting an IC50 value of 28.2 μM. This compound has demonstrated anti-proliferative and apoptotic effects in MCF-7/ADR cancer cell lines, making it a valuable reagent for research in neurobiology and cancer biology. Its ability to modulate cholinergic signaling and induce cell death highlights its potential for further investigation in therapeutic applications.

Cat. No.

A31560

CAS No.

2841473-39-8

ZLMT-12

ZLMT-12 is a potent CDK2/9 inhibitor, demonstrating IC50 values of 0.002 μM and 0.011 μM against CDK9 and CDK2, respectively. This compound is derived from tacrine and exhibits weak inhibition of acetylcholinesterase (IC50 = 19.023 μM) and butyrylcholinesterase (IC50 = 2.768 μM). ZLMT-12 is characterized by low toxicity and notable antiproliferative activity, effectively inducing apoptosis and facilitating cell cycle arrest in the S and G2/M phases. This compound serves as a valuable tool for research in cell cycle regulation and therapeutic development in cancer biology.

Cat. No.

A32002

CAS No.

1433961-56-8

Carbaryl-d3

Carbaryl-d3 is a deuterium-labeled variant of Carbaryl, characterized as an acetylcholinesterase inhibitor. This compound prevents the breakdown of acetylcholine in the synaptic cleft, resulting in its accumulation and subsequent neurotoxic effects. Carbaryl-d3 is employed in research related to neurotoxicity mechanisms and may serve as a tool for studying the pharmacokinetics and metabolic pathways of Carbaryl. Its stable isotope labeling enhances analytical precision in experimental applications.

Cat. No.

A32277

CAS No.

2086689-94-1

Pamiparib maleate

Synonyms: BGB-290 maleate

Pamiparib maleate is a highly potent and selective inhibitor of poly (ADP-ribose) polymerase (PARP), targeting apoptotic pathways. This compound effectively penetrates the blood-brain barrier, inducing neurotoxicity manifesting as cerebral hemorrhage, brain atrophy, and movement disorders in zebrafish embryos. It regulates critical enzymes such as acetylcholinesterase (AChE) and adenosine triphosphatase (ATPase), leading to increased oxidative stress that triggers apoptosis and affects the expression of neurodevelopment-related genes. Additionally, pamiparib maleate downregulates the Notch signaling pathway, providing insights into its potential neurotoxic effects during embryonic development and its relevance in neuropharmacology research.

Cat. No.

A32356

CAS No.

38470-71-2

MAO-B-IN-26

MAO-B-IN-26 is a selective inhibitor of monoamine oxidase B (MAO-B) and acetylcholinesterase, demonstrating neuroprotective properties against β-amyloid (Aβ) induced cytotoxicity in SH-SY5Y cells. This compound effectively mitigates morphological alterations, reactive oxygen species (ROS) generation, and membrane damage associated with neurodegeneration. Additionally, MAO-B-IN-26 suppresses Aβ-induced autophagy and apoptosis, making it a valuable tool for research focused on therapeutic strategies for Alzheimer's disease.

Cat. No.

A32689

CAS No.

1279031-09-2

Galanthamine-O-methyl-d3

Galanthamine-O-methyl-d3 is a deuterium-labeled derivative of Galanthamine, a potent inhibitor of acetylcholinesterase (AChE) with an IC50 value of 500 nM. This stable isotope-labeled compound is primarily utilized in pharmacokinetic and metabolic studies. It serves as a valuable tool for investigating the pharmacological dynamics and biochemical pathways associated with cholinergic activity.

Cat. No.

A32708

CAS No.

362049-56-7

Carbaryl-d7

Carbaryl-d7 is a deuterium-labeled derivative of Carbaryl, which functions as an acetylcholinesterase inhibitor. By suppressing the breakdown of acetylcholine in the synaptic cleft, Carbaryl-d7 leads to an accumulation of acetylcholine, potentially resulting in neurotoxic effects. This stable isotope is primarily utilized in chemical research to study the enzymatic action and biological effects of Carbaryl and its derivatives.

Cat. No.

A32955

CAS No.

2012598-44-4

Galanthamine-d3 hydrochloride

Galanthamine-d3 hydrochloride is a deuterium-labeled derivative of Galanthamine, primarily used as a stable isotope. This compound serves as a useful tool in pharmacokinetic studies and metabolic research, enabling the investigation of drug metabolism and distribution. Galanthamine-d3 hydrochloride plays a significant role in understanding the mechanisms of action of acetylcholinesterase inhibitors and their effects on neurological processes.

Cat. No.

A33946

CAS No.

2390042-05-2

AChE-IN-14

AChE-IN-14 is a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), displaying IC50 values of 0.46 μM for electric eel AChE, 0.48 μM for human recombinant AChE, and 0.44 μM for equine serum BChE. In addition to its cholinesterase inhibition, AChE-IN-14 has a high affinity for the human H3 receptor (H3R) with a Ki value of 159.8 nM. This compound is particularly relevant for research focused on neurodegenerative diseases such as Alzheimer’s disease, where the modulation of cholinergic signaling is critical.

Cat. No.

A34037

CAS No.

14587-50-9

Difeterol

Difeterol is an antihistamine agent that functions primarily as a histamine-1 receptor antagonist. It also inhibits butyrylcholinesterase (BChE), making it a valuable tool for studying cholinergic pathways. This compound is particularly relevant for research related to Alzheimer's disease, where modulation of histamine and cholinergic systems may provide insights into therapeutic strategies.

Cat. No.

A34053

CAS No.

2135615-68-6

Contilisant

Contilisant is a potent antioxidant and neuroprotective agent that targets histamine H3 receptors. It effectively inhibits monoamine oxidases and cholinesterases, contributing to its neuroprotective profile. With a binding affinity of 65.23 nM towards human sigma-1 receptor, Contilisant demonstrates significant therapeutic potential. In preclinical studies, it has been shown to restore cognitive deficits induced by Aβ1-42 in the radial maze assay, making it a valuable tool for Alzheimer's disease research.

Cat. No.

A34117

CAS No.

2756368-79-1

AChE/BChE-IN-21

AChE/BChE-IN-21 is a histamine H3 receptor antagonist that also functions as a calcium channel blocker and acetylcholinesterase inhibitor. This compound demonstrates neuroprotective properties against oxidative stress induced by H2O2 and amyloid-beta peptide Aβ1-40. Additionally, AChE/BChE-IN-21 has been shown to improve cognitive function in mouse models of Alzheimer's disease, making it a valuable tool for research into neurodegenerative disorders.

Cat. No.

A34122

CAS No.

2970985-05-6

H3R antagonist 2

H3R Antagonist 2 is a selective antagonist of the histamine H3 receptor (H3R) with a Ki value of 170 nM for human H3R. This compound demonstrates inhibitory activity against acetylcholinesterase, butyrylcholinesterase, and human monoamine oxidase B (hMAO B), with IC50 values of 180 nM, 880 nM, and 775 nM, respectively. Additionally, H3R Antagonist 2 exhibits promising anti-neuropathic pain and memory-enhancing effects, effectively crossing the blood-brain barrier (BBB). This makes it a valuable tool for research in neuropharmacology and cognitive enhancement studies.

Cat. No.

A35163

CAS No.

1321361-13-0

AChE/BChE/BACE-1-IN-1

AChE/BChE/BACE-1-IN-1 is a potent inhibitor of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and beta-secretase 1 (BACE-1), exhibiting IC50 values of 0.058 μM, 0.082 μM, and 0.115 μM, respectively. This compound demonstrates significant binding affinity for the peripheral anionic site of AChE, facilitates brain penetration, and shows potential in disrupting amyloid-beta (Aβ) aggregates. Additionally, AChE/BChE/BACE-1-IN-1 exhibits neuroprotective properties against Aβ-induced stress and possesses promising antioxidant activity, making it a valuable tool for Alzheimer's disease research and related neurodegenerative studies.

Cat. No.

A35167

CAS No.

2761542-55-4

AChE/BChE-IN-9

AChE/BChE-IN-9 is a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), exhibiting IC50 values of 5.74 μM and 14.05 μM, respectively. In addition to its enzymatic inhibition, AChE/BChE-IN-9 demonstrates antioxidant properties with an IC50 of 57.35 μM and has the ability to chelate iron, potentially mitigating oxidative stress. This compound also influences the aggregation of amyloid β1-42, making it relevant for research in neurodegenerative diseases and gerontology. Its capacity to cross the blood-brain barrier further enhances its suitability for studies focused on central nervous system disorders.

Cat. No.

A35172

CAS No.

2412364-73-7

AChE/GSK-3β-IN-1

AChE/GSK-3β-IN-1 is a dual inhibitor targeting acetylcholinesterase (AChE) and glycogen synthase kinase 3 beta (GSK-3β), demonstrating potent inhibition with IC50 values of 1.2 nM for hAChE, 149.8 nM for hBChE, and 22.4 nM for hGSK-3β. This compound effectively penetrates the blood-brain barrier and displays high selectivity for the CMGC kinase family, particularly binding to the ATP site of DYRK1A. Additionally, AChE/GSK-3β-IN-1 has been shown to inhibit reactive oxygen species (ROS) expression, thereby reducing oxidative stress. It is a valuable tool for research into Alzheimer's disease and related neurodegenerative conditions.

Cat. No.

A35173

CAS No.

1877000-20-8

AChE/BChE/BACE-1-IN-2

AChE/BChE/BACE-1-IN-2 is a potent oral inhibitor of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-site amyloid precursor protein cleaving enzyme 1 (BACE-1), exhibiting IC50 values of 0.069 μM, 0.127 μM, and 0.097 μM, respectively. This compound demonstrates significant binding affinity to the peripheral anionic site of AChE, high brain permeability, and the ability to disassemble amyloid-beta (Aβ) aggregates. Additionally, AChE/BChE/BACE-1-IN-2 provides neuroprotective effects against Aβ-induced stress and possesses noteworthy antioxidant properties, making it suitable for research in neurodegenerative disease models.

Cat. No.

A35560

CAS No.

13161-75-6

Pteryxin

Synonyms: (+)-Pteryxin

Pteryxin is a potent butyrylcholinesterase (BChE) inhibitor (IC50 = 12.96 μg/mL) with additional multi-target mechanisms including inhibition of NF-κB, MAPK, NLRP3 inflammasome activation, and modulation of the Nrf2/ARE pathways. This compound demonstrates significant anti-inflammatory, antioxidant, and osteoclastogenesis inhibitory activities. Pteryxin is suitable for research applications related to inflammatory diseases, osteoporosis, diabetes, and neurodegenerative disorders such as Alzheimer's disease.