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].

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

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

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).

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

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 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).

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].

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].

Acetylcholinesterase (ACHE; EC 3.1.1.7) is a cholinergic enzyme primarily located in neuromuscular junctions and cholinergic chemical synapses, often utilized in biochemical research. It catalyzes the hydrolysis of acetylcholine and other choline esters into acetate and choline, terminating neuronal transmission and signaling between synapses to prevent acetylcholine spread and activation of nearby receptors [1].

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

Demethoxydeacetoxypseudolaric acid B's the metabolic reaction of TDA in vivo is mainly occurred in blood and contributes to be the hydrolysis of plasma esterase to ester bond, as well as the glucosylation reaction.

PEN-866 is a potential agent for controlling early stage tumor growth for non-small cell lung cancer (NSCLC). PEN-866 is a novel esterase-cleavable conjugate of an HSP90i and a topoisomerase I inhibitor, SN-38

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

4-Nitrophenyl palmitate serves as a colorimetric substrate for lipase and esterase, enabling the quantification of enzyme activity through the release and colorimetric detection of 4-nitrophenol at 410 nm following enzymatic hydrolysis. This compound facilitates the characterization of enzyme activity across diverse bacterial and mammalian sources, including Burkholderia and porcine pancreatic lipases.

Vinclozolin M2, an active metabolite of vinclozolin, is generated through successive esterase activity and decarboxylation in C. elegans, as well as decarboxylation in human liver microsomes. It functions as an antagonist to the mineralocorticoid (IC50= 1,400 nM) and androgen receptors (IC50= 0.17 nM), demonstrated in reporter assays with MCF-7 cells. This compound is exclusively sold for research and analytical purposes, tailored for controlled laboratory use, and is not available in bulk sizes.

4-Methylumbelliferyl caprylate (MUCAP) is a fluorogenic substrate for C8 esterase. MUCAP is cleaved by C8 esterase to release the fluorescent moiety 4-methylumbelliferyl (4-MU). 4-MU fluorescence is pH-dependent with excitation maxima of 320 and 360 nm at low (1.97-6.72) and high (7.12-10.3) pH, respectively, and an emission maximum ranging from 445 to 455 nm, increasing as pH decreases.

Zanapezil (TAK-147) is a powerful and selective inhibitor of acetylcholine esterase (AChE). It demonstrates significant and reversible inhibition of AChE activity in rat cerebral cortex homogenates (IC50 = 51.2 nM). Furthermore, Zanapezil exhibits moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. This compound holds promise for the investigation of the initial stages of Alzheimer's disease (AD).

α-Glycosidase-IN-1 (compound MZ7) is a potent inhibitor of α-GLY (α-glycosidase) with an IC50 of 44.72 nM and a Ki of 44.74 nM. It also inhibits human carbonic anhydrase isozymes I (hCA I) and II (hCA II) with IC50 values of 104.87 nM and 100.04 nM, respectively, and acetylcholine esterase (AChE) with an IC50 value of 654.87 nM. α-Glycosidase-IN-1 is applicable in the study of diabetes, Alzheimer's disease, ulcers, heart failure, epilepsy, and various other diseases.

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

The sPLA2-IIA Inhibitor is a cyclic pentapeptide analog of FLSYK, specifically cyclic 2-Nal-Leu-Ser-2-Nal-Arg (c2), which interacts with human IIA phospholipase A2 (hGIIA) to impede its ester bond hydrolyzing function. As part of the esterase superfamily, sPLA2 enzymatically cleaves the sn-2 ester bond in glycerophospholipids, releasing arachidonic acid and lysophospholipids[1].

Clostripain (Clostridiopeptidase B), a proteolytic enzyme derived from Clostridium histolyticum, exhibits esterase, amidase, and protease activities. It is notably specific for cleaving carboxy-terminal arginine residues in proteins [1].

CAY10455, an analog of arachidonoyl ethanolamide (anandamide; AEA), is non-fluorescent extracellularly but exhibits bright fluorescence at 530 nm inside cells due to esterase-mediated cleavage. Its uptake by C6 glioma cells is competitively inhibited by AEA and its analogs, suggesting that CAY10455 and AEA utilize the same transporter. Conversely, CAY10455 also inhibits the uptake of tritiated AEA, further indicating competition for the AEA transporter.

Benastatin C is a polyketide synthase-derived benastatin found in [Streptomyces] with diverse biological activities. It inhibits glutathione S-transferase (GST; IC50 = 24 μg ml for the rat liver enzyme) and the esterase activity of isolated porcine pancreatic lipase (IC50 = 10 μg ml). Benastatin C also increases LPS- or concanavalin A-induced blastogenesis of isolated mouse spleen lymphocytes in a concentration-dependent manner.

Latanoprost is an F-series prostaglandin (PG) analog which has been approved for use as an ocular hypotensive drug. Latanoprost is an isopropyl ester, a prodrug form which is converted to latanoprost (free acid) by endogenous esterase enzymes. The free acid form is 200 times more potent than latanoprost as a ligand for the human recombinant FP receptor. 5-trans Latanoprost (free acid) is an isomer of latanoprost (free acid) wherein the double bond between carbons 5 and 6 has been changed from cis (Z) to trans (E). The trans isomer of latanoprost occurs as an impurity in commercial preparations of the bulk drug product. The present compound was prepared primarily as an analytical standard for detection and quantitation of this impurity. From what can be inferred from the study of other trans isomers of F-type prostaglandins, the biological activity of this isomer is likely to be similar to that of the cis isomer. However, there are no specific published reports on the biological activity, and on reducing intraocular pressure in particular, of 5-trans latanoprost.

KBR 2822 is an inhibitor of esterase.

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

HIV-1 protease-IN-10 (Compound 2) exhibits HIV-1 latency reversing activity (IC50: 0.22 μM), selectively binds to the PKCδ C1b domain (IC50: 0.69 μM), and demonstrates stability against esterase-mediated hydrolysis [1].

AChE-IN-4 is an acetylcholine esterase inhibitor (AChEI) with an IC50 value of 24.1 μM.

CEase-IN-1 (Compound A1H3) is a potent, selective inhibitor of cholesterol esterase (CEase) with an IC50 of 0.36 μM, suitable for hypercholesterolemia research [1].

TEI-9648, an analogue of Vitamin D3 Lactone, acts as a potent and specific antagonist to the vitamin D receptor (VDR). This compound effectively blocks the genomic actions mediated by VDR and the Vitamin D responsive element (VDRE) of 1α,25(OH)2D3. Furthermore, TEI-9648 prevents the differentiation of HL-60 cells induced by 1α,25(OH)2D3, indicating its utility in bone metabolism studies[1][2].

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.