esterase

Cholesterol esterase, also known as bile salt-stimulated lipase and carboxyl ester lipase, is an enzyme responsible for hydrolyzing cholesterol ester into cholesterol and free fatty acid within the intestinal lumen. This enzyme, synthesized and stored in zymogen granules within acinar cells, plays a crucial role in accelerating cholesterol absorption [1] [2].

Carboxylesterase-IN-3 is a potent inhibitor of Carboxylesterase Notum (IC50 ≤ 10 nM).Carboxylesterase-IN-3 has the potential to study cancer diseases.

Carboxylesterase-IN-2 is a potent Carboxylesterase Notum inhibitor (IC50 <= 10 nM).Carboxylesterase-IN-2 has potential for the study of cancer diseases.

Phosphodiesterase 4 (PDE4) inhibitor is an inhibitor of PDE4 with an IC50 value of 0.10 μM for the human recombinant enzyme.

Carboxylesterase-IN-1, a novel pesticide, inhibits carboxylesterase at 50 μg mL, demonstrating inhibitory activity comparable to the established inhibitor (triphenyl phosphate).

Notum pectinacetylesterase-1 is a Notum Pectinacetylesterase inhibitor with IC50 < 0.025 μM.

Pancreatic lipase Carboxylesterase 1-IN-1 (Compound 39) is a potent dual inhibitor of pancreatic lipase (PL) with an IC50 of 2.13 μM and human carboxylesterase 1A (hCES1A) with an IC50 of 0.055 μM.

Carboxylesterases (CESs), carboxylate hydrolases broadly distributed in nature and prevalent in mammalian liver, play a significant role in biochemical research. These enzymes facilitate the hydrolysis of diverse substrates, encompassing esters, thioesters, carbamates, and amides, resulting in the conversion of carboxylic acid esters into their respective alcohols and carboxylic acids [1].

Acetylcholinesterase (ACHE) is an enzyme found in the neuromuscular junction and cholinergic synapses. It catalyzes the hydrolysis of acetylcholine, terminating synaptic neuronal transmission and signal propagation. ACHE can be used for research on biosensors.

Phosphodiesterase 2 (II), a key enzyme prominently involved in the hydrolysis of vital second messengers, cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP), is frequently utilized in biochemical research. This enzyme is expressed across various tissues including the adrenal medulla, brain, heart, platelets, macrophages, and endothelial cells, playing a significant role in the regulation of diverse intracellular processes [1].

Phosphodiesterase (PDE), an enzyme capable of catalyzing the hydrolysis of the 3' ring phosphate bond in cyclic nucleotides, plays a crucial role in biochemical research and acts as a vital regulator in signal transduction processes involving the second messenger molecules cAMP and cGMP. Distinguished by their specificity to cyclic nucleotides, PDEs are categorized into different types ranging from PDE1 to PDE11, presenting potential significance in the study and treatment of various diseases [1].

Sphingomyelin phosphodiesterase, a hydrolase, plays a crucial role in sphingomyelin metabolism by catalyzing the conversion of sphingomyelin into phosphocholine and ceramide. Furthermore, it is instrumental in cellular differentiation, immune and inflammatory responses, as well as intracellular cholesterol trafficking and metabolism [1] [2].

Phosphodiesterase-IN-1 (Compound 7), a phosphodiesterase (PDE) inhibitor, exhibits anti-Plasmodium and antiproliferative activities. It effectively inhibits P. falciparum (strain 3D7) with an IC 50 value of 0.64 μM [1].

Fluorescein diacetate (Di-O-acetylfluorescein) is a cell permeable esterase-substrate for hGSTP1-1.

4,4'-Dimethoxybenzil (p-Anisil) is a human intestinal carboxyl esterase (hiCE) inhibitor( Ki : 70 nM).

Roxatidine Acetate hydrochloride (HOE 760) is a specific and competitive histamin H2-receptor antagonist. It inhibits gastric acid secretion and ulcer formation.

Enocyanin, an anthocyanin extracted from grapes, exhibits inhibitory effects on leucine aminopeptidase, acid phosphatase, γ-glutamyl transpeptidase, and esterase activity.

SMP-028 is a neutral cholesterol esterase (CEase) inhibitor(IC50 : 1.01 μM).

Acetylhydrolase-IN-1 is an inhibitor of the esterase 1-Alkyl-2-acetylglycerophosphocholine (Alkylacetyl-GPC: acetylhydrolase).

Tefinostat (CHR-2845) is a potent monocyte macrophage-targeted histone deacetylase (HDAC) inhibitor that is cleaved to the active acid CHR-2847 by intracellular esterase human carboxylesterase-1 (hCE-1). Tefinostat exhibits antitumor activity and can be used in the study of leukemia and advanced hematologic malignancies.

Diacetinase, a member of the esterase family, catalyzes the hydrolysis of glyceryl diacetate (Diacetin). It is utilized in the measurement of lipase activity.

Diethylumbelliferyl phosphate (DEUP) is a potent and selective inhibitor of cholesterol esterase that does not inhibit protein kinase A activity in vitro. It disrupts steroidogenesis by blocking cholesterol transport to mitochondria in steroidogenic cells, with an IC50 of 11.6 μM. This compound may also limit the absorption of dietary cholesterol.

IR-117-17 is an ionizable cationic amino lipid that targets the airways. It is degradable via esterase cleavage, making it less likely to accumulate with repeated dosing.

SN-35210, an ester analogue of ketamine, is designed to undergo rapid inactivation through esterase-mediated hydrolysis. In experiments, SN-35210 induces the Loss of Righting Reflex (LORR) effect in rats at doses comparable to ketamine.