Pepstatin-Pepstatin-A-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPepstatinCat. No.: HY-P0018CAS No.: 26305-03-3Synonyms: Pepstatin A分式: CHNO分量: 685.89Sequence: IsoValeryl-Val-Val-Sta-Ala-Sta-OHSequence Shortening: IsoVeryl-VV-Sta-A-Sta-OH作靶点: Proteasome; HIV Protease; Autophagy作通路: Metabolic

2、Enzyme/Protease; Autophagy储存式: Powder -80C 2 years-20C 1 yearIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 25 mg/mL (36.45 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.4580 mL 7.2898 mL 14.5796 mL5 mM 0.2916 mL 1.4580 mL 2.9159 mL10 mM 0.1458

3、 mL 0.7290 mL 1.4580 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Pepstatin 由放线 类产的种特异性的天冬氨酸蛋酶 (aspartic proteases) 抑制剂，能够抑制hemoglobin-pepsin，hemoglobin-proctase，casein-pepsin，casein-proctase，casein-acid protease 和1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEhemoglobin-aci

4、d protease 的活性，IC50 值分别为 4.5 nM，6.2 nM，150 nM，290 nM，520 nM 和 260nM；同时可抑制 HIV protease 的活性。IC50 & Target IC50: 4.5 nM (Hemoglobin-pepsin), 6.2 nM (Hemoglobin-proctase), 150 nM (Casein-pepsin), 260 nM(Hemoglobin-acid protease), 290 nM (Casein-proctase), 520 nM (Casein-acid protease) 1体外研究 Pepstatin i

5、s a specific acid protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively 1. Pepstatin (Pepstatin A)inhibit

6、s the recombinant HIV protease with an IC50 of 250 M. Pepstatin shows no effect on cellular proteinsynthesis and probably does not exert severe cell toxicity 2.体内研究 Pepstatin has a very low toxicity, with LD50s of 1090 mg/kg, 875 mg/kg, 820 mg/kg and 450 mg/kg for mice,rats, rabbits, and dogs by i.p

7、. route, and 2000 mg/kg for all species by oral route. Pepstatin (0.5-50 mg/kg,p.o.) suppresses stomach ulceration of the pylorus in ligated Shay rats 1.PROTOCOLCell Assay 2 Pepstatin A is freshly dissolved in DMSO at 7 mM. It is very slowly diluted (1:100) into the medium of HIV-infected H9 suspens

8、ion cultures so that no pepstatin A precipitated (final concentration, 70 M pepstatin Aand 1% DMSO), and the cultures are incubated without change of culture medium for 48 hr. As control,uninfected H9 cells are also incubated with pepstatin and in addition HIV infected and uninfected cells areincuba

9、ted with 1% DMSO but without pepstatin 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Environ Sci Technol. 2017 Dec 5;51(23):13938-13948. Toxicol Appl Pharmacol. 2018 Oct 1;356:159-171. Int J Oncol. 2019 May. Mol Med Rep. 2019 Jan;19(1):4

10、1-50.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Umezawa H, et al. Pepstatin, a new pepsin inhibitor produced by Actinomycetes. J Antibiot (Tokyo). 1970 May;23(5):259-62.2. Seelmeier S, et al. Human immunodeficiency virus has an aspartic-type protease that can be inhibited by pepstatin A. Proc Natl AcadSci U S A. 1988 Sep;85(18):6612-6.McePdfHeightCaution: Product has not been fully v