Amifostine-thiol-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrariesAmifostinethiolCat.No.:HY-137864CASNo.:31098-42-7分⼦式:C₅H₁₄N₂S分⼦量:134.24作⽤靶点:MDM-2/p53作⽤通路:Apoptosis储存⽅式:4°C,protectfromlight,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(protectfromlight,storedundernitrogen)溶解性数据体外实验H2O:250mg/mL(1862.34mM;Needultrasonic)DMSO:<1mg/mL(insolubleorslightlysoluble)MassSolvent1mg5mg10mgConcentration制备储备液1mM7.4493mL37.2467mL74.4934mL5mM1.4899mL7.4493mL14.8987mL10mM0.7449mL3.7247mL7.4493mL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⽅式和期限。BIOLOGICALACTIVITY⽣物活性Amifostinethiol(WR-1065)细胞保护剂Amifostine(HY-B0639)的活性代谢物。Amifostinethiol⼀种具有辐射防护能⼒的细胞保护剂。Amifostinethiol通过JNK依赖的信号通路激活p53[1][2][3]。IC50&Targetp53[2]体外研究Amifostinethiolcanreduceboththedirectanddelayeddetrimentaleffectsofbothhighandlow-LETradiationexposures[1].AmifostinethiolattenuatesboththeDNAdamageandtheG1-phasearrestinducedbyradiation[1].Amifostinethiol(4mM;30minutes)protectsRKO36cellsfromchromosomaldamageanddeathinducedby1/2ionizingradiation[1].Amifostinethiol(4mM;30minutes)protectsirradiatedRKO36cellsfromdelayedgenomicinstability[1].AmifostinethioliscytotoxictoRKO36cellsatmilimolarconcentrations,especiallyaftercontinuoustreatment[1].Amifostinethiolat40μMprotectsRKO36cellsfromdelayedgenomicinstabilitybutnotfromcelldeathandimmediatechromosomaldamage[1].AmifostinethiolactivatesJNKresultinginthephosphorylationofp53atthreonine81[2].AmifostinethiolaffectsphosphorylationoftopoisomeraseIIαleadingtochangesinenzymeactivityandcellcycleprogressioninCHOAA8cells[3].REFERENCES[1].JaroslawDziegielewski,etal.WR-1065,theActiveMetaboliteofAmifostine,MitigatesRadiation-InducedDelayedGenomicInstability.FreeRadicBiolMed.2008Dec15;45(12):1674–1681.[2].OlivierPluquet,etal.ThecytoprotectiveaminothiolWR1065activatesp53throughanon-genotoxicsignalingpathwayinvolvingc-JunN-terminalkinase.JBiolChem.2003Apr4;278(14):11879-87.JBiolChem.2003Apr4;278(14):11879-87.[3].J.S.Murley,etal.WR-1065,anactivemetaboliteofthecytoprotectoramifostine,affectsphosphorylationoftopoisomeraseIIαleadingtochangesinenzymeactivityandcellcycleprogressioninCHOAA8cells.CellProlif.1997Jun;30(6):283–294.McePdfHeightMedChemExpress(MCE)只为有资质