Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEIST5-002Cat.No.:HY-19527CASNo.:13484-66-7Synonyms:N6-Benzyladenosine-5'-phosphate分?式:C??H??N?O?P分?量:437.34作?靶點(diǎn):STAT;Apoptosis作?通路:JAK/STATSignaling;StemCell/Wnt;Apoptosis儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性IST5-002，?種有效的Stat5a/b抑制劑，選擇性地抑制Stat5a/b的轉(zhuǎn)錄活性，IC50值分別為1.5μM(Stat5a)和3.5μM(Stat5b)。IST5-002誘導(dǎo)前列腺癌細(xì)胞和慢性粒細(xì)胞??病(CML)細(xì)胞凋亡(apoptotic)和死亡。IST5-002可?于前列腺癌和慢性粒細(xì)胞??病(CML)的研究。IC50&TargetSTAT5aSTAT5b1.5μM(IC50)3.5μM(IC50)體外研究IST5-002(1.5-25μM,2h)inhibitstranscriptionalactivityofStat5aandStat5binadose-dependentmanner[1].IST5-002(0-40μM,3h)inhibitsBcr-Abl-inducedStat5a/bphosphorylationinK562cells[1].IST5-002(5-100μM,2h)inhibitsStat5a/bphosphorylationinT47Dcells,andinhibitsdimerizationinPC-3cells[1].IST5-002(5-100μM,2h)suppressesStat5nucleartranslocationinPC-3cells,andinhibitsDNAbindingofStat5targetgenesandCOS-7cells[1].IST5-002(2-50μM,48h)reducesexpressionofStat5a/btargetgenes(Bcl-xLandcyclinD1)inCWR22Rv1andLNCaPcells[1].IST5-002(3.1-50μM,72h)inhibitscellgrowththroughinductionofapoptosisinhumanprostatecancercells[1].IST5-002(25-100μM,7days)inducesepithelialcelldeathinpatient-derivedprostatecancersexvivoinorganexplantcultures[1].IST5-002(5μM,24-72h)inhibitsStat5a/bphosphorylationandinducesapoptosisofImatinib(HY-15463)-1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEsensitiveand-resistantCMLcells[1].CellViabilityAssay[1]CellLine:CWR22Rv1,LNCaP,andDU145cellsConcentration:3.1,6.3,12.5,25,50μMIncubationTime:72hResult:Decreasedviablecellsby50%to80%at12.5μM.CellCycleAnalysis[1]CellLine:LNCaPandCWR22Rv1cellsConcentration:6,12,25μMIncubationTime:72hResult:Increasedthefractionofdeadcells(sub-G1)anddecreasedthefractionoflivingcells(G2–M).WesternBlotAnalysis[1]CellLine:Bcr-Abl–positiveK562cellsConcentration:0,1,5,10,20,40μMIncubationTime:3hResult:InhibitedBcr-Abl-inducedStat5a/bphosphorylationat5μM,withoutaffectingBcr-Abltyrosinephosphorylationlevels.Immunofluorescence[1]CellLine:PC-3cellsConcentration:5,10,15.20,40μMIncubationTime:2hResult:InhibitedPrl(Prolactin)-inducednucleartranslocationofStat5.體內(nèi)研究RORγtinverseagonist29(intraperitonealinjection,25-100mg/kg,dailyfor10days)inhibitstumorgrowthinprostatecancerxenograftmodel[1].AnimalModel:Prostatecancer(CWR22Rv1)xenograftmodel[1]Dosage:25,50,and100mg/kg2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEAdministration:Intraperitonealinjection,dailyfor10daysResult:Inducedmassivelossofviabletumorcellsanddeadroundedcellsaccumulation.Inducedcelldeaththroughapoptosis(shownbyfragmentedDNAintumorsections).DecreasednuclearStat5a/bcontentby60%,78%,and90%at25,50,and100mg/kg,respectively.REFERENCES[1].ZhiyongLiao,etal.Structure-BasedScreenIdentifiesaPotentSmallMoleculeInhibitorofStat5a/bwithTherapeuticPotentialforProstateCancerandChronicMyeloidLeukemia.MolCancerTher.2015Aug;14(8):1777-93.McePdfHeightCaution:Producthasnotbeenful