Aldicarb sulfone(Temik sulfone) is a carbamate insecticide; is a cholinesterase inhibitor which prevents the breakdown of acetylcholine in the synapse.
AChE/BChE/BACE-1-IN-2 (Compound 4o) is an orally active inhibitor of AChE, BChE, and BACE-1 with IC50 values of 0.069, 0.127 and 0.097 μM against hAChE, hBChE and hBACE-1, respectively. AChE/BChE/BACE-1-IN-2 shows considerable PAS-AChE binding capability, excellent brain permeation, potential disassembly of Aβ aggregates, and neuroprotective activity against Aβ-induced stress. AChE/BChE/BACE-1-IN-2 has remarkable antioxidant potential[1].
Quinolactacin A1 is a potent acetylcholinesterase (AChE) inhibitor from solid state fermentation of Penicillium citrinum 90648. Quinolactacin A1 can be used for the research of Alzheimer disease[1].
Phenserine ((-)-Eseroline phenylcarbamate) is a derivative of Physostigmine and is a potent, noncompetitive, long-acting and selective AChE inhibitor. Phenserine reduces β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ) formation. Phenserine improves cognitive performance and attenuates the progression of Alzheimer's disease[1][2][3].
RPR121056-d3 is the deuterium labeled RPR121056. RPR121056 is a metabolite of Irinotecan (CPT-11), which is generated by CYP3A4. Irinotecan (CPT-11) is an antineoplastic agent that inhibits topoisomerase type I, causing cell death, and is widely used in the treatment of colorectal cancer. Irinotecan also directly inhibits AChE[1][2].
3-Hydroxycarbofuran, a major metabolite of Carbofuran, is a reversible acetylcholinesterase (AChE) inhibitor[1].
Donepezil Hcl(E-2020) is a noncompetitive acetylcholinesterase inhibitor, which can readily cross the blood brain barrier and increases the concentration of cortical acetylcholine. IC50 Value:Target: AChEIt is known that Donepezil Hydrochloride is a useful tool in the study of Alzheimer's disease. Studies indicate that Donepezil Hydrochloride protects the brain against diisopropylfluorophosphate-induced effects. Studies indicate that Donepezil Hydrochloride selectively inhibits acetylcholinesterase, whereas it has little effect on butyrylcholinesterase. Alternate studies suggest that Donepezil Hydrochloride increases the concentration of extracellular acetylcholine in the cerebral cortex and hippocampus of rats.
ASS234 (ASS-234) is a multitarget, potent, and CNS permeable inhibitor with IC50 of 5.2, 43, 350 and 460 nM for MAO-1, MAO-B, EeAChE and eqBuChE, respectively; inhibits Aβ aggregation, possesses antioxidant properties and protects from Aβ-induced apoptosis in vitro; completely blocks the aggregation mediated by AChE of both Aβ1-42 and Aβ1-40, showing a dual binding site to AChE; ASS234 significantly reduces Aβ1-42-mediated toxicity in SH-SY5Y human neuroblastoma cells, ASS234 is a promising multitarget drug candidates with potential impact for Alzheimer's disease.
Octahydroaminoacridine succinate, a Tacrine analogue, is an acetylcholinesterse (AChE) and butyrylcholinesterase (BChE) inhibitor. Octahydroaminoacridine succinate can be used for Alzheimer's disease (AD) research[1].
MAO-B-IN-26 (Compound IC9) is a MAO-B and acetylcholinesterase inhibitor. MAO-B-IN-26 protects SH?SY5Y cells against Aβ induced cytotoxicity, morphological changes, ROS generation and membrane damage. MAO-B-IN-26 also inhibits Aβ induced autophagy and apoptosis. MAO-B-IN-26 can be used as a neuroprotective agent against Alzheimer’s disease[1].
Galanthaminone (Narwedin) is a competitive and reversible cholinesterase (AChE) inhibitor; is used for the treatment of mild to moderate Alzheimer's disease and various other memory impairments.
AChE/BChE/BACE-1-IN-1 (Compound 4k) is an orally active inhibitor of AChE, BChE, and BACE-1 with IC50 values of 0.058, 0.082 and 0.115 μM against hAChE, hBChE and hBACE-1, respectively. AChE/BChE/BACE-1-IN-1 shows considerable PAS-AChE binding capability, excellent brain permeation, potential disassembly of Aβ aggregates, and neuroprotective activity against Aβ-induced stress. AChE/BChE/BACE-1-IN-1 has remarkable antioxidant potential[1].
Blestrin D is a potent butyrylcholinesterase (BChE) mixed-type inhibitor with an IC50 value of 8.1 μM. Blestrin D can be isolated from Bletilla striata. Blestrin D can be used for the research of Alzheimer's disease (AD)[1].
Acetylshikonin, derived from the root of Lithospermum erythrorhizon, has anti-cancer and antiinflammation activity. Acetylshikonin is a non-selective cytochrome P450 inhibitor against all P450s (IC50 values range from 1.4-4.0 μM). Acetylshikonin is an AChE inhibitor and exhibits potent antiapoptosis activity[1][2][3].
Vincosamide, an alkaloid from Psychotria leiocarpa extract, inhibits the acetylcholinesterase (AChE) activity with anti-inflammatory activity[1].
Pseudocoptisine (Isocoptisine) chloride is a quaternary alkaloid with benzylisoquinoline skeleton, was isolated from Corydalis Tuber. Pseudocoptisine chloride inhibits acetylcholinesterase (AChE) activity with an IC50 of 12.8 μM. Anti-inflammatory and anti-amnestic effects[1][2].
Chikusetsusaponin Ib has anti-Alzheimer's disease activity and is a potent AChE inhibitor[1].
Dihydrowithaferin A (2, 3-dihydrowithaferin A) is a withanolide isolated from Withania somnifera. Dihydrowithaferin A is active against acetylcholinesterase (AChE)[1].
N-p-trans-Coumaroyltyramine is a cinnamoylphenethyl amide isolated from polygonum hyrcanicum, acts as an acetylcholinesterase (AChE) inhibitor with an an IC50 of 122 μM. N-p-trans-Coumaroyltyramine exhibits anti-trypanosomal activity with an IC50 of 13.3 µM for T. brucei rhodesiense[1][2].
Linarin (Buddleoside), isolated from the flower extract of Mentha arvensis, shows selective dose dependent inhibitory effect on acetylcholinesterase (AChE)[1].
BChE-IN-12 (compound 12) is a potent butyrylcholinesterase (BChE) non-competitive inhibitor with an IC50 value of 2.3 μM. BChE-IN-12 can be isolated from Bletilla striata. BChE-IN-12 can be used for the research of Alzheimer's disease (AD)[1].
Territrem B is an irreversible inhibitor of Acetylcholinesterase (AChE) inhibitor. Territrem B is also a fungal meroterpenoid that can be isolated from Aspergillus terreus[1][2].
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[1].
Ambenonium (WIN 8077) dichloride tetrahydrate is an orally active and reversible inhibitor of Acetyicholinesterase (AChE) with high affinity. Ambenonium dichloride tetrahydrate inhibits human AChE with an IC50 value of 0.7 nM (hAChE)[1][2].
MR2938 is a potent AChE inhibitor, with an IC50 of 5.04 μM. MR2938 also suppresses NO production obviously (IC50 = 3.29 μM). MR2938 suppresses the neuroinflammation through blocking MAPK/JNK and NF-κB signaling pathways. MR2938 can be used for Alzheimer’s disease (AD) research[1].
Epi-galanthamine-O-methyl-d3 is the deuterium labeled Epi-galantamine. Epi-galantamine is a diastereomer of Galantamine. Epi-galantamine is an alkaloid isolated from the bulbs and flowers of Caucasian snowdrop (Galanthus woronowii). Epi-galantamine inhibits AChE with an EC50 of 45.7 μM[1][2][3].
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[1].
Chlorpyrifos is an organophosphate insecticide that is classified as a phosphorothionate. The oxon metabolite of Chlorpyrifos is an inhibitor of acetylcholinesterase (AChE), affecting neurological function in insects, humans, and other animals. The Chlorpyrifos oxon (CPO) metabolite is hydrolyzed by the plasma enzyme paraoxonase 1 (PON1), and susceptibility to neurotoxicity associated with CPO exposure is mitigated by PON1 overexpression.
Tanshinone IIA anhydride is a potent and irreversible human carboxylesterase (CE) inhibitor with Ki values of 1.9 nM and 1.4 nM for human CE1 and the human intestinal CE (hiCE), respectively[1].
Acephate-d3 is the deuterium labeled Acephate. Acephate is an anticholinesterase insecticide that produces cholinotoxicity. Acephate displays weak inhibition of rat AChE but potently inhibits cockroach AChE.