Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPurinostatmesylateCat.No.:HY-150109CASNo.:2650188-32-0分?式:C??H??N??O?S分?量:586.62作?靶點(diǎn):HDAC;Apoptosis作?通路:CellCycle/DNADamage;Epigenetics;Apoptosis儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性PurinostatmesylateHDAC的選擇性抑制劑。Purinostatmesylate抑制I型和IIb型HDACs的IC50值在0.81-11.5nM之間。Purinostatmesylate誘導(dǎo)LAMA84和188BL-2細(xì)胞凋亡，響細(xì)胞周期，在體內(nèi)表現(xiàn)出較強(qiáng)的抗??病作?。Purinostatmesylate可?于淋巴細(xì)胞??病的研究。IC50&TargetHDAC1HDAC10HDAC2HDAC30.81nM(IC50)1.1nM(IC50)1.4nM(IC50)1.7nM(IC50)HDAC8HDAC6HDAC5HDAC73.8nM(IC50)11.5nM(IC50)426nM(IC50)590nM(IC50)HDAC9HDAC4HDAC11622nM(IC50)1072nM(IC50)3349nM(IC50)體外研究Purinostatmesylate(1-10μM)inhibitsHDAC1,2,3and8withIC50sof0.81,1.4,1.7and3.8nM,inhibitsHDAC6and10withIC50sof11.5and1.1nM,andinhibitsHDAC4,5,7,9and11withIC50sof1072,426,690,622and3348nM,respectively[1].Purinostatmesylate(0-60nM;24h)inducesapoptosisandaffectscellcycleofLAMA84and188BL-2cells[1].CellProliferationAssay[1]CellLine:LAMA84and188BL-2celllinesConcentration:0-80nM1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEIncubationTime:24,48and72hoursResult:SignificantlyinhibitedcellproliferationofLAMA84and188BL-2cells.ApoptosisAnalysis[1]CellLine:LAMA84and188BL-2celllinesConcentration:0-60nMIncubationTime:24hoursResult:InducedapoptosisofLAMA84and188BL-2cells.CellCycleAnalysis[1]CellLine:LAMA84and188BL-2celllinesConcentration:0-40nMIncubationTime:24hoursResult:Dose-dependentlyblockedcellcycleprogressionatG0/G1phase.WesternBlotAnalysis[1]CellLine:LAMA84and188BL-2celllinesConcentration:0-40nMIncubationTime:24hoursResult:Dose-dependentlyincreasedthe191levelsofAc-H3andAc-H4,anddecreasedHSP90.體內(nèi)研究Purinostatmesylate(5-10mg/kg;i.p.threetimesaweekfor5weeks)effectivelysuppressesleukemiaprogressioninvivo[1].Purinostatmesylate(5-10mg/kg;i.v.threetimesaweekfor8weeks)showspotentlyanti-leukemiaeffectsinBCR-ABL(T315I)-inducedprimaryB-ALLmice[1].AnimalModel:Non-irradiatedC57BL/6recipientmicewithBL-2cellsinjection[1]Dosage:5and10mg/kgAdministration:Intraperitonealinjection;5-10mg/kgthreetimesaweek;forfiveweeksResult:Significantlyprolongedtheoverallsurvivalrateandsuppressedleukemiaprogressionofmice,andnotumorcellwasdetectedafterstoppedtreatment.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEAnimalModel:Non-irradiatedC57BL/6recipientmicewithBL-2secondarytransplantation[1]Dosage:10mg/kgAdministration:Intravenousinjection;10mg/kgthreetimesaweekResult:CompletelyeliminatedGFP+B220+cellsinspleensonday3withtwotimestreatmentandthiscompleteinhibitionwasmaintainedfor26daysdurationoftreatment.AnimalModel:B-ALLmousewithBCR-ABL(T315I)-inducedleukemia[1]Dosage:5and10mg/kgAdministration:Intravenousinjection;5and10mg/kgthreetimesaweek;for8weeksResult:SignificantlyprolongedsurvivalrateofBCR-ABL(T315I)-inducedB-ALLmice.Survivedallmiceaftertreatmentfor42days.REFERENCES[1].YangL,etal.PurinostatMesylateIsaUniquelyPotentandSelectiveInhibitorofHDACsfortheTreatmentofBCR-ABL-InducedB-CellAcuteLymphoblasticLeukemia.ClinCancerRes.2019Dec15;25(24):7527-7539.McePdfHeightCaution:Producthasno