KDM5-IN-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEKDM5-IN-1Cat.No.:HY-100422CASNo.:1628210-26-3分⼦式:C₁₇H₂₀N₆O分⼦量:324.38作⽤靶点:HistoneDemethylase作⽤通路:Epigenetics储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥30mg/mL(92.48mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.0828mL15.4140mL30.8280mL5mM0.6166mL3.0828mL6.1656mL10mM0.3083mL1.5414mL3.0828mL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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。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%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(6.41mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.41mM);Clearsolution3.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.5mg/mL(7.71mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性KDM5-IN-1⾼效选择，有⼝服活性的KDM5抑制剂，IC50值为15.1nM。IC50&TargetIC50:15.1nM(KDM5);EC50:0.34μM(PC9H3K4Me3)[1]体外研究KDM5-IN-1isfoundtopotentlyinhibitKDM5BandKDM5Cisoforms(IC50of4.7and65.5nM,respectively).ItissignificantlylesspotentagainstotherKDMenzymes(1A,2B,3B,4C,5A,6A,7B),inhibitingKDM4CthestrongestwithanIC50of1.9μM.KDM5-IN-1stilldisplaysmorethan100-foldselectivityforKDM4Cvs.KDM5A[1].体内研究Whendosedorallyinmiceat50mg/kgtwiceaday,KDM5-IN-1showsanunboundmaximalplasmaconcentrationCmax>15-foldoveritscellEC50,therebyprovidingarobustchemicalprobeforstudyingKDM5biologicalfunctionsinvivo[1].户使⽤本产品发表的科研⽂献•ActaPharmacolSin.2021Apr13.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LiangJ,etal.Leadoptimizationofapyrazolo[1,5-a]pyrimidin-7(4H)-onescaffoldtoidentifypotent,selectiveandorallybioavailableKDM5inhibitorssuitableforinvivobiologicalstudies.BioorgMedChemLett.2016Aug15;26(16):4036-41.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch