CES2A-IN-2 (compound 14n) is an orally active, highly specific, irreversible and covalent CES2A inhibitor with an IC50 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[1].
Molekulargewicht:
410.51
Formel:
C24H30N2O4
Target-Kategorie:
Carboxylesterase (CES)
Anwendungsbeschreibung:
MCE Product type: Reference compound
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