886992-99-0

中文名称:

886992-99-0

中文同义词:

FAP抑制剂(AC-GLY-BOROPRO)

英文名称:

Ac-Gly-BoroPro

英文同义词:

Ac-Gly-BoroPro;Ac-Gly-BoroPro?, >98%;Boronic acid, B-[(2S)-1-[2-(acetylamino)acetyl]-2-pyrrolidinyl]-

CAS号:

886992-99-0

分子式:

C8H15BN2O4

分子量:

214.03

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

886992-99-0.mol

密度 

1.26±0.1 g/cm3(Predicted)

酸度系数(pKa)

9.72±0.20(Predicted)

生物活性

Ac-Gly-BoroPro是选择性的 FAP 抑制剂，Ki 值为23 nM。

靶点

Ki: 23 nM (FAP)

体外研究

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 (K i =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 (K i =377±18 nM). Ac-Gly-BoroPro inhibits other prolyl peptidases (DPP-7, DPP-8, DPP-9, prolyl oligopeptidase, and acylpeptide hydrolase) with K i 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.