ProductDescription

Appearance:Whitepowder

Molecularformula:C34H63N5O9

Molecularweight:685.9

Structure:1Isovalery-Val-Val-Sta-Ala-Sta

whereSta=statine=(3S,4S)-4-amino-3-

hydroxy-6-methylheptanoicacid

KiforPepsin:2approximately10-10M.

PepstatinAisaninhibitorofacidproteases(aspartylpeptidases).Itformsa1:1complexwithproteasessuchaspepsin,1,2renin,1,2cathepsinD,1,2bovinechymosin,2andproteaseB(Aspergillusniger).3Theinhibitorishighlyselective4anddoesnotinhibitthiolproteases,neutralproteasesorserineproteases.Solublizedγ-secretase5andretroviralprotease6arealsoinhibitedbyPepstatinA.Ithasbeenusedtocharacterizeproteasesfromseveralsources.PepstatinAisthoughttoinhibitbyacollected-substrateinhibitionmechanism.

Thisinhibitorisoftenusedasacomponentinafinalmixturewithotherinhibitors(asinSigmaProteaseInhibitorCocktails).Onerecommendedsetofstocksolutionconcentrationsis:bestatin(1.7mM,selectiveforaminopeptidase),E-64(0.22mM,forcysteineproteases),PepstatinA(2.5mM,foraspartylproteases),AEBSF(18mM,forserineproteases)anddisodiumEDTA(86mM,formetalloproteases).

PreparationInstructions

PepstatinAisonlysparinglysolubleinwater.Itisnormallydissolvedinasolventsuchasethanol,methanol,orDMSOanddilutedintobuffer.Thestocksolutionshouldbeofaconcentrationthatthesolventusedisdilutedatleast1000Xintheworkingsolution.

Ithasbeendissolvedat10mg/mLinethanolwithheat.Theresultingsolutioniscolorless,butmayappearhazy.Toremovehaziness,addupto50μlofglacialaceticacidpermLofethanol.

At25mg/mLDMSOPepstatinAformsaclear,faintyellowsolution.

Stocksolutionsat1mg/mLshouldbestableatleastaweekat4°C.A1mMsolutioninmethanolorDMSOshouldbestableformonthsat–20°C.Ifsolutionsbecomemoreyellowthereagentishydrolyzing.

Aneffectiveworkingconcentrationis1μM,stableforatleastonedayatroomtemperature.10Atypicalworkingconcentrationis0.5-1.0μg/mL.

Storage/Stability

Whenstoredat2-8°Cthisproducthasashelflifeof3years.