Romidepsin-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemERomidepsinCat.No.:HY-15149CASNo.:128517-07-7分⼦式:C₂₄H₃₆N₄O₆S₂分⼦量:540.7作⽤靶点:HDAC;Apoptosis作⽤通路:CellCycle/DNADamage;Epigenetics;Apoptosis储存⽅式:Powder-20°C3years*该产品在溶液状态不稳定，建议您现⽤现配，即刻使⽤。溶解性数据体外实验DMSO:50mg/mL(92.47mM;Needultrasonic)扫描⼆维码，运⽤溶解⽅案计算器获得适合您实验体系的溶解⽅案MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8495mL9.2473mL18.4945mL5mM0.3699mL1.8495mL3.6989mL10mM0.1849mL0.9247mL1.8495mL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；该产品在溶液状态不稳定，建议您现⽤现配，即刻使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶1.请依序添加每种溶剂：10%DMSO40%PEG3005%Tween-8045%salineSolubility:≥2.08mg/mL(3.85mM);Clearsolution此⽅案可获得≥2.08mg/mL(3.85mM，饱和度未知)的澄溶液。以1mL⼯作液为例，取100μL20.8mg/mL的澄DMSO储备液加到400μLPEG300中，混合均匀；向上述体系中加⼊50μLTween-80，混合均匀；然后继续加⼊450μL⽣理盐⽔定容⾄1mL。1/4www.MedChemEwww.MedChemE2.请依序添加每种溶剂：10%DMSO90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(4.62mM);Clearsolution此⽅案可获得≥2.5mg/mL(4.62mM，饱和度未知)的澄溶液。以1mL⼯作液为例，取100μL25.0mg/mL的澄DMSO储备液加到900μL20%的SBE-β-CD⽣理盐⽔⽔溶3.液中，混合均匀。请依序添加每种溶剂：10%DMSO90%cornoilSolubility:≥2.5mg/mL(4.62mM);Clearsolution此⽅案可获得≥2.5mg/mL(4.62mM，饱和度未知)的澄溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。以1mL⼯作液为例，取100μL25.0mg/mL的澄DMSO储备液加到900μL⽟⽶油中，混合均匀。BIOLOGICALACTIVITY⽣物活性Romidepsin(FK228)具有抗肿瘤活性的组蛋⽩去⼄酰化酶(HDAC)抑制剂，抑制HDAC1，HDAC2，HDAC4和HDAC6，IC50值分别为36nM，47nM，510nM和1.4μM。Romidepsin(FK228)由紫⾊杆产⽣，诱导G2/M细胞周期阻滞和凋亡(apoptosis)。IC50&TargetHDAC1HDAC2HDAC4HDAC636nM(IC50)47nM(IC50)510nM(IC50)14000nM(IC50)体外研究Romidepsin(0-72hours;0-80nM)inhibitsproliferationofHCCcellsindose-dependentmanner[2].Romidepsin(0-48hours;0-60nM)leadstoatime-anddose-dependentinductionofcellcyclearrestintheG2/MphaseinHCCcells[2].Romidepsin(0-48hours;0-60nM)promotesapoptosisinHCCcells,increasesc-caspase-3,c-caspase-9,andc-PARPproteinexpression[2].CellProliferationAssay[2]CellLine:HCCcellsConcentration:0nM;10nM;20nM;30nM;40nM;50nM;60nM;70nM;80nMIncubationTime:0hours;12hours;24hours;48hours;72hoursResult:InhibitedHCCcellsproliferation.CellCycleAnalysis[2]CellLine:HCCcellsConcentration:0nM;15nM;30nM;60nMIncubationTime:12hours;24hours;48hoursResult:CausedaG2/Marrest.WesternBlotAnalysis[2]2/4www.MedChemEwww.MedChemECellLine:HCCcellsConcentration:0nM;15nM;30nM;60nMIncubationTime:12hours;24hours;48hoursResult:Increaesdc-caspase-3,c-caspase-9,andc-PARPexpressioninHCCcells.体内研究Romidepsin(intraperitonealinjection;0.5and1mg/kg;every3day;21days)inhibitedthetumorgrowth,revealsahigherexpressionofp-cdc25C,ki67,c-caspase-3andc-PARP,andalowerexpressionofKi-67inRomidepsintreatedtumors[2].AnimalModel:NudemicewithHuh7cells[2]Dosage:0.5and1mg/kgAdministration:Intraperitonealinjection;0.5and1mg/kg;every3day;21daysResult:Suppressedtumorgrowthinmousexenograftmodels.户使⽤本产品发表的科研⽂献•CancerRes.2020Oct15;80(20):4426-4438.•CancerRes.2016Dec1;76(23):7001-7011.•Theranostics.2021Mar20;11(11):5605-5619.•CellDeathDis.2020Sep18;11(9):778.•CellDeathDis.2020Sep15;11(9):753.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].FurumaiR,etal.FK228(depsipeptide)asanaturalprodrugthatinhibitsclassIhistonedeacetylases.CancerRes.2002Sep1;62(17):4916-21.[2].SunWJ,etal.RomidepsininducesG2/MphasearrestviaErk/cdc25C/cdc2/cyclinBpathwayandapoptosisinductionthroughJNK/c-Jun/caspase3pathwayinhepatocellularcarcinomacells.BiochemPharmacol.2017Mar1;127:90-100.McePdfHeight3/4www.MedChemEwww.MedChemE关注MCE中国公众号，

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