Suberoyl-bis-hydroxamic-acid-Suberohydroxamic-acid-DataSheet-生命科学试剂-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemESuberoylbis-hydroxamicacidCat.No.:HY-W009776CASNo.:38937-66-5Synonyms:Suberohydroxamicacid;SBHA分⼦式:C₈H₁₆N₂O₄分⼦量:204.22作⽤靶点:HDAC作⽤通路:CellCycle/DNADamage;Epigenetics储存⽅式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(244.83mM;Needultrasonic)H2O:8.33mg/mL(40.79mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM4.8967mL24.4834mL48.9668mL5mM0.9793mL4.8967mL9.7934mL10mM0.4897mL2.4483mL4.8967mL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。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，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(12.24mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(12.24mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoil1/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(12.24mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Suberoylbis-hydroxamicacid(Suberohydroxamicacid;SBHA)竞争性且可透过细胞的HDAC1和HDAC3抑制剂，ID50值分别为0.25μM和0.30μM。Suberoylbis-hydroxamicacid使肿瘤细胞易于凋亡(apoptosis)并促进线粒体凋亡途径。Suberoylbis-hydroxamicacid可⽤于甲状腺髓样癌(MTC)的研究。IC50&TargetHDAC1HDAC30.25μM(IC50)0.30μM(IC50)体外研究Suberoylbis-hydroxamicacid(10,20or50μM;24hours)combinationwithTRAILimprovesapoptosisextent,andwhenTRAILiscombinedwith20μMSBHA(itselfcausingonly10–15%apoptosis),resultingin45–50%celldeath[1].Suberoylbis-hydroxamicacid(20-50μM;10-20hours)alonehaslittleeffectontheexpressionoftheproteinsBcl-xL,Mcl-1,andhasalbeitmildeffectonBax.WhenitcombineswithTRAIL,whichincreasestheratioofrelativeproteinexpressionofBcl-xLandBaxinearlyperiods,whilethechangeintheratioofMcl-1andBaxincreaseslaterinMM-BIandIst-Mes2cells[1].Suberoylbis-hydroxamicacid(30μM;6hours)causesaccumulationofacetylatedhistoneH4inMELcells[2].ApoptosisAnalysis[1]CellLine:MM-BIandIst-Mes2cellsConcentration:10μM,20μMor50μMIncubationTime:24hoursResult:Showedacooperativeeffectincellapoptosis.体内研究Suberoylbis-hydroxamicacid(intraperitonealinjection;200mg/kg;every2days;12days)revealsamarkedincreaseintheactiveformofNotch1(NICD)withaconcomitantdecreaseinASCL1.ItreducestheMTCtumorgrowth[3].AnimalModel:NudemiceinjectedwithhumanMTCcells[3]Dosage:200mg/kgAdministration:Intraperitonealinjection;every2days;12daysResult:Resultedinanaverage55%inhibitionoftumorgrowthinSBHAtreatmentgroup.REFERENCES[1].JiriNeuzil,etal.SensitizationofMesotheliomatoTRAILApoptosisbyInhibitionofHistoneDeacetylase:RoleofBcl-xLDown-2/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemERegulation.BiochemBiophysResCommun.2004Jan30;314(1):186-91.[2].VMRichon,etal.AClassofHybridPolarInducersofTransformedCellDifferentiationInhibitsHistoneDeacetylases.ProcNatlAcadSciUSA[3].LiNing,etal.SuberoylBishydroxamicAcidActivatesnotch1SignalingandSuppressesTumorProgressioninanAnimalModelofMedullaryThyroidCarcinoma.AnnSurgOncol.2008Sep;15(9):2600-5.McePdfHeightCaution:Producthasnotbe