human carboxylesterase

Temocapril is an inhibitor of tyrosine kinase.

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

Benzil is a bioactive aromatic ketone commonly used as a photoinitiator in polymer chemistry, exhibiting inhibitory activity against human carboxylesterase (hCE1) in Sf21 cells.

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.

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.

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].

Isolicoflavonol is a potential cancer chemopreventive agent.