Ac-Gly-BoroPro |
| Catalog No.GC32883 |
Ac-Gly-BoroPro est un inhibiteur sélectif de la FAP avec un Ki de 23 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 886992-99-0
Sample solution is provided at 25 µL, 10mM.
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Ac-Gly-BoroPro is a selective FAP inhibitor with a Ki of 23 nM.
FAP has been implicated in cancer; however, its specific role remains elusive because inhibitors that distinguish FAP from other prolyl peptidases like dipeptidyl peptidase-4 (DPP-4) have not been developed. Ac-Gly-BoroPro selectively inhibits FAP relative to other prolyl peptidases. FAP reacts readily with submicromolar concentrations of Ac-Gly-BoroPro, reaching steady state inhibition levels rapidly (Ki=23±3 nM). In contrast, DPP-4 requires higher Ac-Gly-BoroPro concentrations for inhibition and a longer time to reach steady state inhibition levels (Ki=377±18 nM). Ac-Gly-BoroPro inhibits other prolyl peptidases (DPP-7, DPP-8, DPP-9, prolyl oligopeptidase, and acylpeptide hydrolase) with Ki values ranging from 9- to 5400-fold higher than that for FAP inhibition. The N-acyl-linkage in Ac-Gly-BoroPro blocks the N terminus of the inhibitor, making it less nucleophilic and therefore unlikely to cyclize[1].
[1]. Edosada CY, et al. Selective inhibition of fibroblast activation protein protease based on dipeptide substrate specificity. J Biol Chem. 2006 Mar 17;281(11):7437-44.
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