Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemE(Rac)-Z-FA-FMKCat.No.:HY-123185CASNo.:96922-64-4分子式:C??H??FN?O?分子量:386.42作用靶點(diǎn):Cathepsin;Caspase;SARS-CoV;InterleukinRelated;NF-κB作用通路:MetabolicEnzyme/Protease;Apoptosis;Anti-infection;Immunology/Inflammation;NF-κB儲(chǔ)存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性(Rac)-Z-FA-FMK是Z-FA-FMK的外消旋體。(Rac)-Z-FA-FMK是組織蛋白酶B的抑制劑，其Ki為1.5μM。(Rac)-Z-FA-FMK可抑制caspase-2、-3、-6、-7和-9，其IC50分別為6.147、15.41、32.45、9.077和110.7μM。(Rac)-Z-FA-FMK可抑制SARS-CoV-2復(fù)制的主要蛋白酶，其IC50為11.39μM。(Rac)-Z-FA-FMK可抑制巨噬細(xì)胞中LPS誘導(dǎo)的IL-1β水平升高和NF-κB轉(zhuǎn)錄激活[1][2][3][4]。REFERENCESSmith,R.A.,etal.,(1988).InhibitionofcathepsinBbypeptidylaldehydesandketones:slow-bindingbehaviorofatrifluoromethylketone.Biochemistry,27(17),6568–6573.Lopez-Hernandez,F.J.,etal.,(2003).Z-FA-fmkinhibitseffectorcaspasesbutnotinitiatorcaspases8and10,anddemonstratesthatnovelanticancerretinoid-relatedmoleculesinduceapoptosisviatheintrinsicpathway.Molecularcancertherapeutics,2(3),255–263.Zhu,W.,etal.,(2020).IdentificationofSARS-CoV-23CLProteaseInhibitorsbyaQuantitativeHigh-ThroughputScreening.ACSpharmacology&translationalscience,3(5),1008–1016.Schotte,P.,etal.,(2001).ThecathepsinBinhibitorz-FA.fmkinhibitscytokineproductioninmacrophagesstimulatedbylipopolysaccharide.TheJournalofbiologicalchemistry,276(24),21153–21157.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;021-58955