Esterase Inhibitors

By Targets:	Apoptosis (1) Bacterial (2) Cholinesterase (ChE) (5) Dopamine Receptor (2) EAAT (1) HDAC (1) Lipase (1) MetAP (1) Phospholipase (1)
By Research Areas:	Cancer (2) Inflammation/Immunology (1) Metabolic Disease (4) Neurological Disease (5)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-103610

4,4'-Dimethoxybenzil

p-Anisil
Others Cancer

4,4'-Dimethoxybenzil is a human intestinal carboxyl esterase (hiCE) inhibitor with K_i of 70 nM.
HY-124258

Valilactone

(-)-Valilactone
Others Metabolic Disease

Valilactone is a potent and effective inhibitor of esterase, produced by actinomycetes .
HY-156984

Monometacrine

Others Neurological Disease

Monometacrine is a cholesterol esterase inhibitor. Monometacrine has antidepressant effect .
HY-19861

SMP-028

SMP-028 is an inhibitor of neutral cholesterol esterase (CEase), with an IC₅₀ of 1.01 μM.

4,4'-Dimethoxybenzil p-Anisil	Others	Cancer
4,4'-Dimethoxybenzil is a human intestinal carboxyl esterase (hiCE) inhibitor with K_i of 70 nM.

Valilactone (-)-Valilactone	Others	Metabolic Disease
Valilactone is a potent and effective inhibitor of esterase, produced by actinomycetes .

Monometacrine	Others	Neurological Disease
Monometacrine is a cholesterol esterase inhibitor. Monometacrine has antidepressant effect .

SMP-028
SMP-028 is an inhibitor of neutral cholesterol esterase (CEase), with an IC₅₀ of 1.01 μM.

CEase-IN-1	Cholinesterase (ChE)	Metabolic Disease
CEase-IN-1 (Compound A1H3) is a potent and selective cholesterol esterase (CEase) inhibitor with an IC₅₀ of 0.36 μM. CEase-IN-1 can be used for the research of hypercholesterolemia .

Tefinostat 1 Publications Verification CHR-2845	HDAC Apoptosis	Cancer
Tefinostat (CHR-2845) is a monocyte/macrophage targeted histone deacetylase (HDAC) inhibitor. Tefinostat can be cleaved into active acid CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1). Tefinostat can be used for the research of leukaemias .

TAOA AM Ester trimethyl lock	EAAT	Neurological Disease
TAOA AM Ester trimethyl lock is a high-affinity fluorescent prodrug-like inhibitor of the excitatory amino acid transporter (EAAT). It can penetrate the cell membrane and be activated by hydrolysis by endogenous cell esterases to form active EAAT inhibitors. TAOA AM Ester trimethyl lock can be used to study neurodegeneration and neuronal cell death .

Itopride hydrochloride HSR803	Cholinesterase (ChE) Dopamine Receptor Bacterial	Neurological Disease
Itopride (HSR803) hydrochloride is a potent dopamine-2 antagonist and an *acetylcholine esterase* (AChE)** inhibitor. Itopride hydrochloride enhances gastric motility through both antidopaminergic and anti-acetylcholinesterasic actions, can be used as a gastrointestinal prokinetic agent. Itopride can be used for researching gastro-esophageal reflux disease (GERD) .

Ebelactone A	Lipase MetAP	Others Inflammation/Immunology
Ebelactone A is a mycolic acid β-lactone, which exhibits inhibitory activity for *esterase, lipase, fMet aminopeptidase (fMet AP) and PNBase, with IC₅₀s of 56, 3, 8 and 7.5 μM, respectively . Ebelactone A inhibits* cutinase, exhibits plants protective potency against Erysiphe graminis .

Itopride HSR803 free base	Cholinesterase (ChE) Dopamine Receptor Bacterial	Others
Itopride (HSR803 free base) is a potent and orally active dopamine-2 antagonist and an *acetylcholine esterase* (AChE)** inhibitor. Itopride enhances gastric motility through both antidopaminergic and anti-acetylcholinesterasic actions, can be used as a gastrointestinal prokinetic agent. Itopride can be used for researching gastro-esophageal reflux disease (GERD) .

AA26-9	Phospholipase	Metabolic Disease
AA26-9 is a potent and broad spectrum serine hydrolase inhibitor. AA26-9 targets included serine peptidases, lipases, amidases, esterases, and thioesterases. AA26-9 shows inhibitory activity against approximately 1/3 of the 40+ serine hydrolases detected in immortalized T cell lines .

Zanapezil fumarate TAK-147 fumarate	Cholinesterase (ChE)	Neurological Disease
Zanapezil (TAK-147) fumarate is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil fumarate shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC₅₀=51.2 nM). Zanapezil fumarate shows a moderate inhibition of muscarinic M1 and M2 receptor binding with K_i values of 234 and 340 nM, respectively. Zanapezil fumarate can be used for the research of early stages of Alzheimer's disease (AD) .

Zanapezil free base TAK-147 free base	Cholinesterase (ChE)	Neurological Disease
Zanapezil (TAK-147) free base is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil free base shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC₅₀=51.2 nM). Zanapezil free base shows a moderate inhibition of muscarinic M1 and M2 receptor binding with K_i values of 234 and 340 nM, respectively. Zanapezil free base can be used for the research of early stages of Alzheimer's disease (AD) .

Cat. No.	Product Name	Target	Research Area

sPLA2-IIA Inhibitor	Peptides	Metabolic Disease
sPLA2-IIA Inhibitor is a cyclic pentapeptide analog of FLSYK (cyclic 2-Nal-Leu-Ser-2-Nal-Arg (c2)), that binds to hGIIA (human IIA phospholipase A2) and inhibits its hydrolytic ability. sPLA2 is a member of the esterase superfamily that catalyzes the hydrolysis of the ester bond at the sn-2 position of glycerophospholipids, releasing free fatty acids such as arachidonic acid and lysophospholipids .

Cat. No.	Product Name	Category	Target	Chemical Structure

Valilactone (-)-Valilactone	Alkaloids Microorganisms Classification of Application Fields Source classification Metabolic Disease Disease Research Fields	Others
Valilactone is a potent and effective inhibitor of esterase, produced by actinomycetes .

Ebelactone A	Structural Classification Natural Products Microorganisms Source classification	Lipase MetAP
Ebelactone A is a mycolic acid β-lactone, which exhibits inhibitory activity for *esterase, lipase, fMet aminopeptidase (fMet AP) and PNBase, with IC₅₀s of 56, 3, 8 and 7.5 μM, respectively . Ebelactone A inhibits* cutinase, exhibits plants protective potency against Erysiphe graminis .

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