carboxylesterase

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].

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.

Ethyl phenylglyoxylate (AI3 10033) is a simultaneous inhibitor and substrate of chicken liver carboxylesterase.

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.

Irinotecan Hydrochloride (CPT-11 hydrochloride) is the hydrochloride salt of a semisynthetic derivative of camptothecin. Irinotecan, a prodrug, is converted to a biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38) by a carboxylesterase-converting enzyme. One thousand-fold more potent than its parent compound irinotecan, SN-38 inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death. Because ongoing DNA synthesis is necessary for irinotecan to exert its cytotoxic effects, it is classified as an S-phase-specific agent.

Temocapril is an inhibitor of tyrosine kinase.

Phoxim is an organophosphate insecticide that inhibits acetylcholinesterase (AchE) activity in the nervous system of insects. It is used in veterinary medicine for the treatment of ectoparasitic mites. It is toxic to aquatic organisms and may affect cytochrome P450 enzyme (CYP1A) activity and its expression levels in fish liver microsomes. In addition, sub-lethal doses of phoxim affected detoxification enzyme activities of adult mulberry whitefly, such as changes in the activities of glutathione S-transferase (GST), carboxylesterase (CarE) and acetylcholinesterase (AchE).

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.

Antifeedant agent 1 functions as a carboxylesterase inhibitor that controls insect pests by inhibiting their feeding, with an EC50 of 0.038 mg mL. It is applicable in the research of pest control.

Tributyl phosphite is an alkyl phosphite. It is reported to inhibit carboxylesterase activity.

2,4-D-methyl is a carboxylesterase in herbicide bioactivation.

Cytochrome P450 metabolites of arachidonic acid, such as 11(12)-EpETrE and 14(15)-EpETrE have been identified as endothelium derived hyperpolarizing factors with vasodilator activity. Soluble epoxide hydrolase (sEH) catalyzes the conversion of EpETrEs to the corresponding DiHETrEs thereby diminishing their activity. Inhibitors of sEH may therefore have clinical utility for treating hypertension and systemic inflammation. S-NEPC is a colorimetric substrate used to measure sEH activity. It also is a substrate for Glutathione S-transferase, microsomal epoxide hydrolase and porcine liver carboxylesterase. Hydrolysis of S-NEPC by sEH yields 4-nitrophenol which can be quantified spectrophotometrically at 405 nm. S-NEPC is adaptable for use in 96-well microwell plate readers.

Oseltamivir acid methyl ester is a precursor form of oseltamivir acid, which is converted to oseltamivir acid by carboxylesterase 1 (CES1). Oseltamivir acid, in turn, acts as a neuraminidase inhibitor and antiviral agent [1].

Oseltamivir acid methyl ester hydrochloride is a precursor form of oseltamivir acid. Oseltamivir acid methyl ester is converted to oseltamivir acid converted by carboxylesterase 1 (CES1).

Temocapril hydrochloride (CS-622 HCl), the hydrochloride of Temocapril, is a long-acting ACE inhibitor used for the therapy of hypertension.

1. Fraxinellone significantly reduced weight loss and diarrhea in mice and alleviated the macroscopic and microscopic signs of the disease. 2. Fraxinellone exhibited a variety of insecticidal activities including feeding-deterrent activity, inhibition of growth, and larvicidal activity. 3. Fraxinellone has effect in the midgut metabolism of Mythimna separata (M. separata), via protease (especially the weak alkaline trypsin-like enzyme), carboxylesterase and glutathione S-transferase.

Benz-AP, a potent photosensitizer, generates singlet oxygen inversely related to Human carboxylesterase 2 (hCES2) activity, showcasing enhanced photocytotoxicity in cancer cells within low hCES2 environments. Moreover, upon Two-photon excitation (TPE), Benz-AP induces the production of reactive oxygen species (ROS), effectively killing cancer cells and tumor spheroids [1].

Tanshinone IIA anhydride is a potent, irreversible inhibitor of human carboxylesterase (CE), exhibiting inhibitory constants (K i values) of 1.9 nM for human CE1 and 1.4 nM for human intestinal CE (hiCE), respectively [1].

Compound 44 (hCES2A-IN-2) is an orally active inhibitor of human carboxylesterase 2 (hCES2A) with an IC50 of 5.02 μM, which ameliorates Irinotecan-induced delayed diarrhea [1].

hCES2-IN-1 (Compound 24) is a reversible and selective inhibitor of the human carboxylesterase 2 (hCES2) enzyme, with an IC50 of 6.72 μM. This compound reduces hCES2 levels in vivo and is effective in treating irinotecan-induced delayed diarrhea and DSS-induced ulcerative colitis [1].

Irinotecan-d10 Hydrochloride is a deuterated compound of Irinotecan Hydrochloride. Irinotecan Hydrochloride has a CAS number of 100286-90-6. Irinotecan Hydrochloride is the hydrochloride salt of a semisynthetic derivative of camptothecin. Irinotecan, a prodrug, is converted to a biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38) by a carboxylesterase-converting enzyme. One thousand-fold more potent than its parent compound irinotecan, SN-38 inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death. Because ongoing DNA synthesis is necessary for irinotecan to exert its cytotoxic effects, it is classified as an S-phase-specific agent.

Isolicoflavonol is a potential cancer chemopreventive agent.