AChE

Cat. No.

A26257

CAS No.

480-36-4

Linarin

Synonyms: Buddleoside; Linarine

Linarin is a selective inhibitor of acetylcholinesterase (AChE), demonstrating oral bioavailability. This compound exhibits a range of biological activities, including anti-inflammatory, antioxidant, sedative, and antibacterial properties. Linarin is valuable for research in neurological disorders, osteoporosis, and cancer, providing insights into potential therapeutic applications across these areas.

Cat. No.

A26422

CAS No.

2925457-33-4

BChE/HDAC6-IN-2

BChE/HDAC6-IN-2 is a potent dual inhibitor targeting both butyrylcholinesterase (BChE) and histone deacetylase 6 (HDAC6), demonstrating IC50 values of 1.8 nM and 71.0 nM, respectively. This compound exhibits significant neuroprotective properties and scavenges reactive oxygen species (ROS), alongside effectively chelating metal ions such as Fe2+ and Cu2+. Furthermore, BChE/HDAC6-IN-2 inhibits tau phosphorylation and presents moderate immunomodulatory effects, making it a valuable reagent for research into neurodegenerative diseases and related pathways.

Cat. No.

A26442

CAS No.

2414053-06-6

AChE/HDAC-IN-1

AChE/HDAC-IN-1 is a potent dual inhibitor of acetylcholinesterase (AChE) and histone deacetylases (HDAC) with IC50 values of 0.12 nM and 0.23 nM, respectively. This compound also demonstrates antioxidant activity and metal chelating properties, making it a valuable tool in understanding neurodegenerative processes. AChE/HDAC-IN-1 is suitable for research applications related to Alzheimer's disease and other conditions associated with cholinergic dysfunction and epigenetic modifications.

Cat. No.

A26469

CAS No.

2413603-15-1

HDAC6-IN-5

HDAC6-IN-5 is a potent inhibitor of histone deacetylase 6 (HDAC6), demonstrating an IC50 of 0.025 μM. This compound effectively inhibits the self-aggregation of amyloid-beta 1-42 and acetylcholinesterase (AChE), with IC50 values of 3.0 μM and 0.72 μM, respectively. HDAC6-IN-5 has been shown to promote neurite outgrowth while exhibiting minimal neurotoxicity, making it a valuable tool for research in neurodegenerative disease and neuronal regeneration studies.

Cat. No.

A26478

CAS No.

2413603-10-6

HDAC6-IN-6

HDAC6-IN-6 is a potent inhibitor of histone deacetylase 6 (HDAC6), exhibiting an IC50 of 0.025 μM. This compound is capable of crossing the blood-brain barrier and demonstrates strong inhibitory activity against amyloid-beta peptide (Aβ1-42) self-aggregation and acetylcholinesterase (AChE) with IC50 values of 3.0 μM and 0.72 μM, respectively. Additionally, HDAC6-IN-6 enhances neurite outgrowth while maintaining a favorable safety profile, making it a valuable tool for research in neurodegenerative diseases and related fields.

Cat. No.

A26503

CAS No.

2925457-27-6

BChE/HDAC6-IN-1

BChE/HDAC6-IN-1 is a selective dual inhibitor targeting both butyrylcholinesterase (BChE) and histone deacetylase 6 (HDAC6), with IC50 values of 4 nM and 8.9 nM, respectively. This compound demonstrates significant potential in ameliorating cognitive impairment in an Aβ1–42-induced mouse model, making it a valuable tool in Alzheimer's disease research. Its ability to modulate both cholinergic and epigenetic pathways positions BChE/HDAC6-IN-1 as a promising candidate for studies focused on neurodegenerative disorders.

Cat. No.

A28354

CAS No.

638-97-1

β-Amyrone

Synonyms: β-Amyron

β-Amyrone is a triterpene compound recognized for its anti-inflammatory properties, primarily through the inhibition of cyclooxygenase-2 (COX-2) expression. It demonstrates significant antifungal activity and exhibits antiviral effects against the Chikungunya virus. Additionally, β-Amyrone inhibits α-glucosidase and acetylcholinesterase (AChE) activities, making it a valuable compound for research in inflammation, infectious diseases, and obesity-related studies.

Cat. No.

A29625

CAS No.

444667-97-4

BGC-201259

Synonyms: RS-1259

BGC-201259 is a potent and orally active inhibitor of acetylcholinesterase (AChE) and serotonin transporter (SERT), with IC50 values of 101 nM and 42 nM, respectively. Additionally, it inhibits the 5-HT receptor with an IC50 of 90 nM. BGC-201259 exhibits varying activity against several targets, including the norepinephrine transporter (IC50 = 7.7 μM), L-type calcium channel (IC50 = 3.6 μM), σ receptor (IC50 = 2 μM), and sodium channel (IC50 = 5.1 μM). This compound shows promise in research related to Alzheimer's disease by potentially enhancing cognitive and emotional functions through its dual-targeting mechanism.

Cat. No.

A29715

CAS No.

1639925-34-0

Flucopride

Flucopride is an AChE inhibitor with an IC50 of 24 nM, demonstrating significant potency in acetylcholinesterase modulation. Additionally, it acts as a partial agonist at the 5-HT4 receptor with a binding affinity (Ki) of 9.6 nM. Flucopride facilitates non-amyloidogenic processing of amyloid precursor protein (APP) in COS-7 cells expressing the human 5-HT4 receptor, with an EC50 of 23.0 nM. Its properties suggest effective gastrointestinal tract penetration and the capability to cross the blood-brain barrier, as indicated by PAMPA assay results, making it relevant for neuropharmacology research.

Cat. No.

A30082

CAS No.

115066-04-1

α-NETA

α-NETA is a potent noncompetitive inhibitor of choline acetyltransferase (ChA), exhibiting an IC50 value of 9 μM. Additionally, it displays strong antagonistic activity against aldehyde dehydrogenase 1A1 (ALDH1A1) with an IC50 of 0.04 µM and also targets chemokine-like receptor-1 (CMKLR1). While it shows some inhibitory effects on cholinesterase (ChE) and acetylcholinesterase (AChE) with higher IC50 values, α-NETA is notable for its anti-cancer properties, making it a valuable tool for research in cancer biology and neuropharmacology.

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.

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.

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.

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.

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.

Cat. No.

A35996

CAS No.

2766380-73-6

Y13g

Y13g is a potent dual inhibitor of acetylcholinesterase (AChE) and interleukin-6 (IL-6). By targeting these pathways, Y13g demonstrates significant potential in addressing memory deficits associated with Alzheimer’s Disease. In preclinical studies, Y13g effectively reverses memory impairment induced by STZ and exhibits histopathological profiles akin to those of healthy specimens, making it a valuable tool for research in neurodegeneration and inflammatory responses.

Cat. No.

A35998

CAS No.

3077831-11-6

BChE/p38-α MAPK-IN-1

BChE/p38-α MAPK-IN-1 is a selective dual inhibitor targeting human butyrylcholinesterase (BChE) with an IC50 of 772 nM and p38 α MAPK with an IC50 of 191 nM. This compound significantly reduces the production of pro-inflammatory cytokines such as IL-1β, IL-6, IL-8, and TNF-α in cellular models. BChE/p38-α MAPK-IN-1 demonstrates the potential to ameliorate cognitive impairments induced by scopolamine and alleviate spatial learning deficits in LPS-treated mice, making it a valuable tool for studying Alzheimer's disease by addressing cholinergic deficits and neuroinflammation.