carboxylesterase-in-2

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

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].

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].

Isolicoflavonol is a potential cancer chemopreventive agent.

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.

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].