Ac-Gly-BoroPro-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAc-Gly-BoroProCat. No.: HY-101801CAS No.: 886992-99-0分式: CHBNO分量: 214.03Sequence: Ac-Gly-boroProSequence Shortening: Ac-G-boroP作靶点: Others作通路: Others储存式: Powder -80C 2 years-20C 1 yearIn solvent -80C 6 months-20C 1 month溶解性数据体外实

2、验 DMSO : 50 mg/mL (233.61 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 4.6722 mL 23.3612 mL 46.7224 mL5 mM 0.9344 mL 4.6722 mL 9.3445 mL10 mM 0.4672 mL 2.3361 mL 4.6722 mL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，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Ac-Gly-BoroPr

3、o是选择性的 FAP 抑制剂，Ki 值为23 nM。IC50 & Target Ki: 23 nM (FAP) 11/2 Master of Small Molecules 您边的抑制剂师www.MedChemE体外研究 FAP has been implicated in cancer; however, its specific role remains elusive because inhibitors thatdistinguish FAP from other prolyl peptidases like dipeptidyl peptidase-4 (DPP-4) have no

4、t been developed.Ac-Gly-BoroPro selectively inhibits FAP relative to other prolyl peptidases. FAP reacts readily withsubmicromolar concentrations of Ac-Gly-BoroPro, reaching steady state inhibition levels rapidly (Ki=233nM). In contrast, DPP-4 requires higher Ac-Gly-BoroPro concentrations for inhibi

5、tion and a longer time toreach steady state inhibition levels (Ki=37718 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-foldhigher than that for FAP inhibition. The N-acyl-linkage in Ac

6、-Gly-BoroPro blocks the N terminus of theinhibitor, making it less nucleophilic and therefore unlikely to cyclize 1.PROTOCOLKinase Assay 1 Ki values for inhibition of proteases by Ac-Gly-BoroPro are determined using the method of progress curvesfor analysis of tight binding competitive inhibitors. V

7、arious concentrations of Ac-Gly-BoroPro are reacted withFAP (1.0 nM) and DPP-4 (0.1 nM) in the presence of Ala-Pro-AFC (500 M for FAP; 100 M for DPP-4), andtime-dependent inhibition of each protease is monitored. Reactions contained inhibitor concentrations at least20-fold greater than protease conc

8、entrations, such that the protease-inhibitor complex does not significantlydeplete the free inhibitor 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. 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.McePdfHeightCaution: Product has not been fully validated for medical applicat