carboxylesterase-in-1

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.

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.

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].

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].

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].

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].