AChE Inhibitor

AChE/BChE-IN-18 (Compound 4g) is a dual inhibitor of AChE/BChE , with a IC₅₀ value of 0.315 μM for AchE. AChE/BChE-IN-18 is also a CB2R antagonist with a K_i value of 31 nM. AChE/BChE-IN-18 has neuroprotective activity.

GFAP/NF-κB/APOE/NLRP3-IN-1 is an orally active, blood-brain barrier-permeable multi-target inhibitor with an IC₅₀ of 3.50 nM against Acetylcholinesterase. GFAP/NF-κB/APOE/NLRP3-IN-1 inhibits BACE-1 with an IC₅₀ of 14.61 nM. GFAP/NF-κB/APOE/NLRP3-IN-1 inhibits Aβ_1-42 aggregation with an IC₅₀ of 8.63 μM. GFAP/NF-κB/APOE/NLRP3-IN-1 reduces the levels of GFAP, NLRP3 inflammasome, NF-κB and APOE. GFAP/NF-κB/APOE/NLRP3-IN-1 is applicable for the research of Alzheimer's disease and neuroblastoma.

AChE-IN-81 (compound 22) is a potent, irreversible and selective AChE inhibitor. AChE-IN-81 inhibits activity on AChE with inhibitory rates of 80.0%, with an IC₅₀ of 3.7 μM. AChE-IN-81 binds to AChE with a binding affinity (K_d) of 5.37 μM. AChE-IN-81 effectively reduces in zebrafish brain cells. AChE-IN-81 exhibits potential neuroprotective activities on H₂O₂-induced SH-SY5Y cell injury model.

BuChE-IN-22 is a pseudo-irreversible butyrylcholinesterase (BuChE) inhibitor, with IC₅₀ values of 4 nM and 157 nM against hBuChE and hAChE, respectively. It also acts as a prodrug of 7-hydroxysertraline. BuChE-IN-22 releases 7-hydroxysertraline during BuChE inhibition. BuChE-IN-22 completely reverses Aβ_25-35-induced short-term and long-term memory impairments in a mouse model of Alzheimer's disease. BuChE-IN-22 can be used in research related to Alzheimer's disease.

AChE-IN-60 (compound 6k) is a potant acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitor with IC₅₀s of 27 nM and 43 nM, respectively. AChE-IN-60 also inhibits monoamine oxidase (MAO)-A and MAO-B with IC₅₀s of 353 nM and 716 nM, respectively.

Echothiopate iodide (Echothiophate iodide) is an acetylcholinesterase (AChE) inhibitor. Echothiopate iodide irreversibly inhibits acetylcholinesterase, prevents the enzymatic hydrolysis of acetylcholine, and increases the local acetylcholine concentration in the ciliary muscle, thereby driving muscarinic receptor downregulation and regulatory hyposensitivity to Pilocarpine Hydrochloride. Echothiopate iodide can be used in the study of glaucoma.

BChE/p38-α MAPK-IN-2 is a BChE and p38-α MAPK dual inhibitor. BChE/p38-α MAPK-IN-2 inhibits hBChE with an IC₅₀ of 5.1 nM, showing 1000-fold selectivity over hAChE. BChE/p38-α MAPK-IN-2 inhibits p38α MAPK with an IC₅₀ of 8.12 μM. BChE/p38-α MAPK-IN-2 exhibits neuroprotective effect and can be used for the research of neurological disease, such as Alzheimer’s disease.

BChE-IN-55 is a reversible competitive inhibitor of butyrylcholinesterase (BChE) and acetylcholinesterase (AChE), with IC₅₀ values of 2.91 μM (eqBChE) and 34.42 μM (eeAChE), respectively. BChE-IN-55 exhibits antioxidant activity. BChE-IN-55 can be used for research on Alzheimer's disease.

Azamethiphos is an acetylcholinesterase inhibitor and insecticide. Azamethiphos covalently binds to acetylcholinesterase via phosphorylation, inhibits its activity, causes acetylcholine to accumulate in cholinergic synapses, triggers uncontrolled excitation of cholinergic sites, induces paralysis and leads to death. Azamethiphos can be used as a bath insecticide in salmonid aquaculture to control sea lice infestations, and it exerts acute toxicity to European lobster larvae, including mortality and movement disorders.

Propoxur-d₃ is the deuterated form of Propoxur (HY-B0916). Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests.

AChE-IN-44 (Compound Tap4) is an AChE inhibitor. AChE-IN-44 can be converted into the thiazole salt AChE inhibitor Tat2.

BChE-IN-3 (compound 45a) is a potent, selective, time-dependent and pseudoirreversible BChE inhibitor, with an IC₅₀ of 56.9 nM. BChE-IN-3 also shows marginal and reversible (not time-dependent) inhibition of AChE.

AChE-IN-28 (Compound 2h) is a selective slow-binding inhibitor of acetylcholinesterase with an IC₅₀ of 0.2 nM.

Dihydroconiferyl dihydro-p-coumarate is a mesophenolic acetylcholinesterase (AChE) inhibitor discovered in orchids such as Vanda roxburghii and Dendrobium nobile, with an IC₅₀ of 118.17 μg/mL against mouse AChE. Dihydroconiferyl dihydro-p-coumarate reduces the hydrolytic activity of AChE, scavenges DPPH and hydroxyl radicals, exhibits potassium ferricyanide reducing power, reduces Mo (VI) to Mo (V), and inhibits lipid peroxidation in mouse brain homogenates. Dihydroconiferyl dihydro-p-coumarate is a key hypoglycemic compound and shows no significant cytotoxicity to human cancer cells. Dihydroconiferyl dihydro-p-coumarate can be used in research related to Alzheimer's disease and type 2 diabetes.

AChE/BChE-IN-30 (Compound 3g) is a Cholinesterase dual-target competitive inhibitor. AChE/BChE-IN-30 can inhibit AChE and BChE with IC₅₀ values of 0.338 and 2.087 μM and K_i values of 0.045 and 0.789 μM. AChE/BChE-IN-30 can be used for the research of neurological disease, such as Alzheimer's disease.

ChEs/MAOs-IN-2 (compound a11) is a cholinesterases and monoamine oxidases inhibitor with IC₅₀ values of 0.10, 0.20, 0.30, 0.40 µM for MAO-A, MAO-B, AChE, and BChE, respectively. ChEs/MAOs-IN-2 has the potential for the research of Alzheimer's disease.

Asoxime dimesylate (HI-6 dimesylate) is an orally active thiosemicarbazone-based antidote. Asoxime dimesylate is a reversible inhibitor of AChE, and its core mechanism of action is to re-activate AChE inhibited by nerve toxins, thereby restoring the cholinergic nerve function. Asoxime dimesylate significantly restores the function of poisoned muscles without reactivating AChE. Asoxime dimesylate is an antagonist of acetylcholine receptors (AChRs), including nicotinic receptor and α7 nAChR. Asoxime dimesylate can serve as an effective immunomodulator, improving the immune effect of the nervous system.

Isogarcinol (Cambogin) is a potent AChE and BChE inhibitor, with IC₅₀ values of 1.13 and 8.30 μM, respectively. Isogarcinol also shows leishmanicidal activity, with an IC₅₀ of 0.33 μM against L. donovani.

hBChE-IN-4 (compound 40) is a potent hCA activator and BChE inhibitor with K_A values of 266, 76.9, 918, 893, 98.0 nM for hCA I, hCA II, hCA IV, hCA VB, hCA VII, IC₅₀ values of 72.1, 4.2 nM for eeAChE, eqBChE, respectively. hBChE-IN-4 shows no cytotoxicity. hBChE-IN-4 shows potent procognitive effects. hBChE-IN-4 has the potential for the research of neurodegenerative diseases and other neuropsychiatric disorders.

Scutellarein 4'-methyl ether 7-O-glucuronide (Clerodendroside) is a flavonoid inhibitor of acetylcholinesterase (AChE) (IC₅₀=1 mg/mL). Scutellarein 4'-methyl ether 7-O-glucuronide can be isolated from Plectranthus barbatus. It also possesses antioxidant activity and can be used in research on neurological diseases such as Alzheimer's disease.