CES2A-IN-2 (compound 14n) is an orally active, highly specific, irreversible and covalent CES2A inhibitor with an IC 50 of 0.04 nM for human CES2A. CES2A-IN-2 covalently binds to CES2A by specifically targeting the catalytic serine residue (Ser-228). CES2A-IN-2 can significantly ameliorate Irinotecan -triggered gut toxicity (ITGT) without diminishing the anti-tumor effects of Irinotecan ( HY-16562 ) in tumor-bearing mice.
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