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Ac-Gly-BoroPro  ≥98%

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包装规格：1mg 5mg in glass bottle
溶解性：溶于DMSO（≥50mg/mL）
产品描述：基本信息 产品编号： A12655 产品名称： Ac-Gly-BoroPro CAS: 886992-99-0   储存条件 粉末 -20℃ 四年     分子式： C8H15BN2O4 溶于液体     分子量 214.03     化学名：  [1-(N-Acetylglycyl)pyrrolidine-2beta-yl]boronic acid Solubility (25°C)：   体外:   DMSO ≥50mg/mL(233.61mM) Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 4.6722mL 23.3612mL 46.7224mL 5mM 0.9344mL 4.6722mL 9.3445mL 10mM 0.4672mL 2.3361mL 4.6722mL   生物活性 产品描述 一种选择性的 FAP 抑制剂，Ki 值为23nM。 靶点 Ki: 23nM (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 (Ki=23±3nM). In contrast, DPP-4 requires higher Ac-Gly-BoroPro concentrations for inhibition and a longer time to reach steady state inhibition levels (Ki=377±18nM). 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 特征     推荐实验方法(仅供参考) Kinase Assay Ki values for inhibition of proteases by Ac-Gly-BoroPro are determined using the method of progress curves for analysis of tight binding competitive inhibitors. Various concentrations of Ac-Gly-BoroPro are reacted with FAP (1.0nM) and DPP-4 (0.1nM) in the presence of Ala-Pro-AFC (500μM for FAP; 100μM for DPP-4), and time-dependent inhibition of each protease is monitored. Reactions contained inhibitor concentrations at least 20-fold greater than protease concentrations, such that the protease-inhibitor complex does not significantly deplete the free inhibitor
保存条件：-20℃

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