AChE Inhibitor

Methylene Violet 3RAX is a phenazine dye to stain the mitochondria of cells. Methylene Violet 3RAX can change the molecular structure of DNA, undermine the module of DNA, and induce the generation of the reactive singlet oxygen. Methylene Violet 3RAX shows inhibition for human erythrocyte AChE and human plasma BChE with an K_is of 1.58, 0.51 μM, respectively. Methylene Violet 3RAX has the potential for the research of potential photosensitizers for mitochondrial targeting action in PDT (photodynamic therapy).

Isoprocarb is carbamate insecticide that widely used to control rice paddy lice and leafhopper. Isoprocarb is also an AChE inhibitor.

Picfeltarraenin IB, a triterpenoid obtained from Picriafel-terrae Lour (P.fel-terrae), is an acetylcholinesterase (AChE) inhibitor. Picfeltarraenin IB can be used for the treatment of herpes infections, cancer and inflammation.

Fenchlorphos, an organophosphate, is an insecticide. Fenchlorphos is an inhibitor of the enzyme acetylcholinesterase (AChE). Fenchlorphos is able to cause mitochondrial dysfunction.

Ladostigil (TV-3326) hydrochloride is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC₅₀s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil hydrochloride exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil can be used for the research of depression and Alzheimer's disease. Ladostigil (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Ebeiedinone, a steroidal alkaloid from Fritillaria species, inhibits the bioactivity of human whole blood cholinesterase (ChE) at the concentration of 0.1 mM, with the inhibitory effects of 69.0%.

AChE-IN-65 (Compound DABA_1) is a mixed inhibitor for acetylcholinesterase (AChE), with a K_i of 556.4 μM for Electrophorus electricus AChE.

Acotiamide monohydrochloride trihydrate is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with IC₅₀ of 1.79 μM. Acotiamide monohydrochloride trihydrate can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide monohydrochloride trihydrate has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory .

Pirimicarb is a fast-acting selective carbamate insecticide on a wide range of crops including cereals, sugar beet, potatoes, fruits and vegetables. Pirimicarb is an AChE inhibitor and an acaricide.

PCS1055 is a selective and competitive antagonist for muscarinic M4 receptor with an IC₅₀ of 18.1 nM and a K_d of 5.72 nM. PCS1055 inhibits radioligand [³H]-NMS binding to the M4 receptor with a K_i of 6.5 nM. PCS1055 is also an inhibitor for AChE with IC₅₀ of 22 nM and 120 nM for electric eel and human AChE, respectively.

Y13g dihydrochloride 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 dihydrochloride reverses the STZ (HY-13753)-induced memory deficit, and shows histopathology similarly as in normal animals.

Dihydrowithaferin A (2, 3-dihydrowithaferin A) is a withanolide isolated from Withania somnifera. Dihydrowithaferin A is active against acetylcholinesterase (AChE).

BChE-IN-17 (compound 6n) is a potent and selective BChE inhibitor with IC₅₀s of 10.5 nM and 32.5 nM for eqBChE and hBChE, respectively. BChE-IN-17 shows over 1000-fold selectivity to BChE against AChE. BChE-IN-17 shows low neurotoxicity and moderate neuroprotective effects.

Sophoflavescenol is a prenylated flavonol, which shows great inhibitory activity with IC₅₀ of 0.013 μM against Phosphodiesterase 5 (PDE5), and also inhibits RLAR, HRAR, AGE, BACE1, AChE and BChE with IC₅₀s of 0.30 μM, 0.17 μM, 17.89 μg/mL, 10.98 μM, 8.37 μM and 8.21 μM, respectively.

ASS234 is a potent monoamino oxidase (MAO) inhibitor with IC₅₀s of 5.2 nM and 43 nM for MAO-A and MAO-B, respectively. ASS234 also inhibits AChE and BuChE with IC₅₀s of 350 nM and 460 nM, respectively.

Ebelin lactone is an acetylcholinesterase (AChE) inhibitor, with a K_i of 0.45 μM against human M1 muscarinic acetylcholine receptor (mAChR) and a K_i of 4.21 μM against human 5-HT2A serotonin receptor. Ebelin lactone binds to the allosteric cavity above the orthosteric site of M1 via nonpolar interactions with subtype-selective residues. Ebelin lactone binds to the cavity between transmembrane helices 4 and 5 of 5-HT2A through nonpolar interactions with orthosteric site residues. Ebelin lactone exhibits free radical scavenging activity, inhibits cancer cell proliferation, and regulates memory and cognitive processes by interacting with M1 and 5-HT2A receptors. Ebelin lactone can be used in studies related to Alzheimer's disease, breast cancer and colorectal cancer.

Isorosmanol is an abietane-type diterpene isolated from Rosmarinus officinalis L. aerial parts, with antioxidant, neuroprotective and neurotrophic effects. Isorosmanol inhibits AChE activity and melanin synthesis.

Phosalone is an orally active, blood-brain barrier penetrant Insecticide and acaricide. Phosalone inhibits the activity of Acetylcholinesterase. Phosalone acts as a substrate for detoxifying esterases. Phosalone induces symptoms of cholinergic hyperactivity, toxic reactions, mortality, oxidative stress, and changes in pro-inflammatory protein levels, and exerts toxic effects on colonic tissues and cells. Phosalone controls pistachio psyllids. Phosalone can be used in studies related to colitis.

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.