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human cholinesterases

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By Targets:	Carboxylesterase (CES) (2) Cholinesterase (ChE) (8) Drug Metabolite (1) Histamine Receptor (1) Monoamine Oxidase (1) Reactive Oxygen Species (ROS) (1)
By Research Areas:	Cancer (1) Inflammation/Immunology (2) Metabolic Disease (2) Neurological Disease (7)

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-N10686

Tanshinone IIA anhydride	Carboxylesterase (CES)	Cancer
Tanshinone IIA anhydride, present in root extracts of Salvia miltiorrhiza, acts as an inhibitor of human carboxylesterase (CE). Tanshinone IIA anhydride has a K_i value of 1.9 nM against hCE1 and a K_i value of 1.4 nM against hiCE. Tanshinone IIA anhydride forms a stable covalent complex with serine Ser221 at the active site of hCE1, blocking the catalytic cycle of carboxylesterase, and the activity of the inactivated enzyme cannot recover spontaneously. Tanshinone IIA anhydride is applicable in metabolism-related studies .

HY-107275

Ebeiedinone	Cholinesterase (ChE)	Neurological Disease
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% .

HY-16252

Hexafluorenium dibromide Mylaxen	Cholinesterase (ChE)	Neurological Disease
Hexafluorenium dibromide (Mylaxen) is a potent cholinesterase (ChE) inhibitor with pI₅₀ value of 6.96 and K_i value of 2.4 nM for human plasma cholinesterase (ChE) .

HY-151562

AChE/BuChE/MAO-B-IN-1	Cholinesterase (ChE) Monoamine Oxidase	Neurological Disease
AChE/BuChE/MAO-B-IN-1 (compound 19) is an inhibitor of human acetyl- (hAChE), butyrylcholinesterase (hBuChE) and monoamine oxidase-B (hMAO-B) with IC₅₀s of 4.8 μM, 13.7 μM, and 1.11 μM, respectively. AChE/BuChE/MAO-B-IN-1 also exhibits high affinity to both the σ₁ and σ₂ receptors with K_i values of 42.8 nM (human σ₁ receptor) and 191 nM (rat σ₂ receptor), respectively. AChE/BuChE/MAO-B-IN-1 can be used for Alzheimer’s disease research .

HY-124446

Dibromsalicil	Carboxylesterase (CES)	Metabolic Disease
Dibromsalicil (Compound 31) is a carboxylesterase (CES) inhibitor with activity of 72.7 nM against hiCE (human intestinal carboxylesterase) and 53.5 nM against rCE (rabbit liver carboxylesterase). Dibromsalicil has almost no activity against hCE1 (human liver carboxylesterase) and cholinesterase .

HY-157437

AChE/BChE-IN-16	Cholinesterase (ChE) Reactive Oxygen Species (ROS)	Neurological Disease Inflammation/Immunology
AChE/BChE-IN-16 (compound C7) is a potent cholinesterase (ChE) inhibitor with IC₅₀s of 30 nM and 48 nM for human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBChE), respectively. AChE/BChE-IN-16 exhibits a remarkable capacity to safeguard PC12 cells against H₂O₂-induced apoptosis and effectively suppresses the production of reactive oxygen species (ROS) .

HY-146035

AChE-IN-14	Cholinesterase (ChE) Histamine Receptor	Neurological Disease
AChE-IN-14 (compound 5) is a potent cholinesterase inhibitor with IC₅₀s of 0.46 , 0.48, and 0.44 μM for electric eel acetylcholinesterase (eeAChE), human recombinant acetylcholinesterase (hAChE), and equine serum butyrylcholinesterase (eqBuChE), respectively. AChE-IN-14 exhibits high affinity toward human H₃ receptor (H₃R; K_i= 159.8 nM). AChE-IN-14 can be used for the research of Alzheimer’s disease .

HY-149300

SB-1436	Cholinesterase (ChE)	Neurological Disease
SB-1436 is an *Cholinesterase* (ChE) inhibitor, inhibits acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and recombinant human acetylcholinesterase (rHuAChE) with IC₅₀s of 0.176, 0.37 and 0.08 μM, respectively. SB-1436 inhibits AChE and BChE in a non-competitive manner with K_is of 0.046 and 0.115 μM, respectively. SB-1436 significantly stops the self-aggregation of Aβ, and can be used for neurological disease research .

HY-172219

CUR-IPA	Cholinesterase (ChE)	Neurological Disease Inflammation/Immunology
CUR-IPA is a *cholinesterase* inhibitor, with IC₅₀ of 5.99, 59.30, and 60.66 μM for eAChE (electric eel), hAChE (human), and hBChE (human), respectively. CUR-IPA can scavenge free radicals and has antioxidant activity. CUR-IPA can be used in the research of cognitive dysfunction .

HY-183750

BChE reactivator-1	Cholinesterase (ChE)	Metabolic Disease
BChE reactivator-1 is a human butyrylcholinesterase (BChE) activator and antidote, with a K_i value of 0.52 μM against human BChE. BChE reactivator-1 activates BChE inhibited by organophosphorus compounds, binds reversibly to native BChE, and restores cholinesterase activity in human whole blood. BChE reactivator-1 is applicable to research related to organophosphorus poisoning .

HY-W741033

Demeton-S sulfone	Drug Metabolite	Others
Demeton-S sulfone is an oxidative metabolite of the organophosphorus insecticide Disulfoton .

Tanshinone IIA anhydride	Structural Classification Flavonoids Labiatae Samanea saman (Jacq.) Merr. Plants Other Flavonoids Source Classification	Carboxylesterase (CES)
Tanshinone IIA anhydride, present in root extracts of Salvia miltiorrhiza, acts as an inhibitor of human carboxylesterase (CE). Tanshinone IIA anhydride has a K_i value of 1.9 nM against hCE1 and a K_i value of 1.4 nM against hiCE. Tanshinone IIA anhydride forms a stable covalent complex with serine Ser221 at the active site of hCE1, blocking the catalytic cycle of carboxylesterase, and the activity of the inactivated enzyme cannot recover spontaneously. Tanshinone IIA anhydride is applicable in metabolism-related studies .

Ebeiedinone	Alkaloids Piperidine Alkaloids Liliaceae Plants Fritillaria ussuriensis Maxim. Source Classification	Cholinesterase (ChE)
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% .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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human cholinesterases

Inhibitors & Agonists

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