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.

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].

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].

Isolicoflavonol is a potential cancer chemopreventive agent.