Cholinesterase (ChE) Inhibitor

(E)-2-Nitrocinnamic acid (Compound 1k) is an Acetylcholinesterase inhibitor. (E)-2-Nitrocinnamic acid is applicable to research related to Alzheimer's disease.

Dual AChE-MAO B-IN-1 (compound 15) is an orally bioavailable CNS-permeant potent inhibitor of both human AChE (IC₅₀=550 nM) and MAO B (IC₅₀=8.2 nM). Dual AChE-MAO B-IN-1 behaves as a safe and metabolically stable neuroprotective agent, devoid of cytochrome liability.

AChE/BChE-IN-29 is an AChE/BChE inhibitor. AChE/BChE-IN-29 exhibits balanced dual cholinesterase inhibitory activity with IC₅₀ values of 2.1 μM for Electrophorus electricus AChE (eeAChE) and 6.3 μM for equine serum butyrylcholinesterase (eqBChE). AChE/BChE-IN-29 effectively inhibits amyloid-β (Aβ₄₂) aggregation and tau protein aggregation in E. coli cell models. AChE/BChE-IN-29 can be used for the study of Alzheimer’s disease (AD).

hiCE inhibitor-1, a sulfonamide derivative, is a selective human intestinal enzyme (hiCE) inhibitor with a K_i value of 53.3 nM. hiCE inhibitor-1 can be used to improve Irinotecan (HY-16562)-induced diarrhoea.

DCDQ is a potent acetylcholinesterase (AChE) inhibitor. DCDQ shows a strong binding affinity with the 4EY7 protein (binding energy: −8.2 kcal/mol). DCDQ is promising for research of Alzheimer's disease (AD).

BuChE-IN-9 (compound 22a) is a potent equine serum-derived BuChE (eqBuChE) inhibitor with an IC₅₀ of 173 nM. BuChE-IN-9 also inhibits human BACE1, Aβ aggregation, mouse GABA transporter 1 (mGAT1) and mGAT4. BuChE-IN-9 has significant antiamnesic properties.

Aβ-IN-5 (Compound e12) is an orally active Aβ aggregation inhibitor. Aβ-IN-5 also inhibits AChE and BuChE with IC₅₀ values of 21.29 μM and 1.32 μM, respectively. Aβ-IN-5 shows excellent neuroprotective effects and low neurotoxicity.

AChE/BChE-IN-8 (Compound 5a) is an uncompetitive AChE and mixed BChE inhibitor with K_i values of 0.788 μM and 2.364 μM against Electrophorus electricus AChE (EeAChE) and equine BChE (eqBChE), respectively. AChE/BChE-IN-8 can cross the BBB and has low cytotoxicity.

RX 67668 is a potent cholinesterase inhibitor with an IC₅₀ of 5 μM for both acetylcholinesterase (AChE) and butyrylcholinesterase. RX 67668 can reverse the neuromuscular blockade induced by D-tubocurarine. RX 67668 is a muscle relaxant used to relieve skeletal muscle fatigue.

Lanuginosine is an alkaloid. Lanuginosine can be isolated from the stems of Xylopia laevigata (Annonaceae) and the leaves of Magnolia grandiflora. Lanuginosine induces Apoptosis. Lanuginosine inhibits AChE (IC₅₀: 10.9 μM). Lanuginosine inhibits Aβ aggregation. Lanuginosine exhibits anticancer activity against hepatocellular carcinoma, human promyelocytic leukemia, human chronic myeloid leukemia, melanoma, and brain tumors. Lanuginosine can be used in the research of Alzheimer's disease.

AChE/BChE/MAO-B-IN-3, an indan-1-one derivative, is a potent MAO-B inhibitor with an IC₅₀ of 0.0359 μM for human MAO-B. AChE/BChE/MAO-B-IN-3 is a potent AChE and BChE enzyme inhibitor, with IC₅₀s of 0.0473 μM and 0.0782 μM for human AChE and BChE enzyme, respectively. AChE/BChE/MAO-B-IN-3 shows significant antioxidant activity and has the potential for Alzheimer's disease (AD) research.

Dehydrogeijerin is an inhibitor of acetylcholinesterase with an IC₅₀ of 9.7 μM. Dehydrogeijerin can be used in study Alzheimer’s disease.

Ilicicolin C exhibits antibacterial activity against Pseudomonas syringae with IC₅₀ of 28.5 µg/mL. Ilicicolin C exhibits weak inhibitory activities against acetylcholinesterase (AChE) and β-glucuronidase with IC₅₀ of 30-43 µg/mL. Ilicicolin C exhibits weak cytoxicity in human lung fibroblasts with IC₅₀ of 64-120 µg/mL. Ilicicolin C affects seed germination and root tip growth of lettuce.

AChE-IN-86 (Compound 6f) is an inhibitor of enzyme acetylcholinesterase (AChE) with IC₅₀ values of 25.33 μg/mL. AChE-IN-86 exerts inhibitory activity against AChE through forming hydrogen bonds, π-π and π-alkyl interactions with amino acid residues at the key catalytic sites of AChE. AChE-IN-86 can be used for Alzheimer's disease study.

hBChE-IN-2 (compound 15d) is a butyrylcholinesterase (BChE) inhibitor (IC₅₀ of 0.62 μM) and a cannabinoid receptor 2 (CB2R) agonist. hBChE-IN-2 has neuroprotection activities.

Paecilomide is a pyridone alkaloid and acetylcholinesterase inhibitor.

Y13g is the potent inhibitor of both AChE and IL-6. Interleukin-6 (IL-6) and acetylcholinesterase (AChE) are two important targets implicated in progression of Alzheimer's Disease (AD). Y13g reverses the STZ (HY-13753)-induced memory deficit, and shows histopathology similarly as in normal animals.

Dimethyl sulfoxide (suitable for HPLC) is an aprotic solvent that can dissolve water-insoluble therapeutic and toxic agents. Dimethyl sulfoxide (DMSO) has a strong affinity for water and has the ability to rapidly penetrate or enhance the penetration of other substances through biological membranes. Dimethyl sulfoxide also has potential free radical scavenging and anticholinesterase effects and may affect coagulation activity. Dimethyl sulfoxide also induces histamine release from mast cells but is thought to have low systemic toxicity. Dimethyl sulfoxide (suitable for HPLC) is suitable for HPLC.

Phoxim-d5 (phenyl-d5) (mixture of isomers) is the deuterated-labeled Phoxim (HY-B0819). Phoxim is an organophosphorus pesticide and an orally active inhibitor of cholinesterase and CYP3A, which induces neurotoxicity in Caenorhabditis elegans and causes nephrotoxicity characterized by glomerular atrophy and interstitial fibrosis. Phoxim induces inhibition of the autophagy pathway. Phoxim induces dopaminergic neuron degeneration and exacerbates Aβ-induced paralysis. Phoxim damages enterocytes and disrupts intestinal barrier integrity. Phoxim induces ROS accumulation. Phoxim induces mitochondrial apoptosis, involving upregulation of Bad, Bax, caspase-3, and caspase-9 and downregulation of Bcl-2. Phoxim inhibits mitochondrial functional enzymes (COX, Ca²⁺-Mg²⁺-ATPase, SDH). Phoxim upregulates Nrf2 mRNA expression in the jejunal mucosa. Phoxim increases TNF-α and decreases IL-6 and IL-8 in the intestinal mucosa. Phoxim alters gut microbial composition by increasing total bacteria and Escherichia coli and reducing Lactobacillus. Phoxim enhances energy metabolism in silver carp by upregulating key glycolytic and gluconeogenic enzymes. Phoxim is used in research on neurodegenerative diseases, nephrotoxicity, intestinal oxidative stress and barrier dysfunction, and bacterial sepsis.

AChE/Aβ-IN-2 (compound 33) is a potent and orally active inhibitor of acetylcholinesterase (AChE) with IC₅₀ of 135 nM, as well as an antagonist of NMDA receptor (GluN1-1b/GluN2B subunit combination) with IC₅₀ of 5.054 μM. AChE/Aβ-IN-2 also inhibits Aβ aggregation and shows good blood-brain barrier permeability. AChE/Aβ-IN-2 improves cognitive and spatial memory impairment in rats model.