hCES2A-IN-2 (compound 14n) is an orally active, highly specific, irreversible, covalent inhibitor of hCES2A with an IC50 of 0.04 nM. It targets and covalently binds to the catalytic serine residue (Ser-228) of hCES2A. hCES2A-IN-2 can significantly mitigate irinotecan-induced gastrointestinal toxicity (ITGT) without diminishing the antitumor efficacy of irinotecan in tumor-bearing mice.
Target-Kategorie:
Lipid
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