GSK-J1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGSK-J1Cat.No.:HY-15648CASNo.:1373422-53-7分⼦式:C₂₂H₂₃N₅O₂分⼦量:389.45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:50mg/mL(128.39mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5677mL12.8386mL25.6772mL5mM0.5135mL2.5677mL5.1354mL10mM0.2568mL1.2839mL2.5677mL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%salineSolubility:≥2.5mg/mL(6.42mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.42mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性GSK-J1H3K27me3/me2-demethylasesJMJD3/KDM6B和UTX/KDM6A的抑制剂，对KDM6B的IC50值为60nM。IC50&TargetIC50:60nM(KDM6B)[2]体外研究GSK-J1isselectiveforH3K27demethylasesoftheKDM6subfamilyandspecificallybindstoendogenousJMJD3.GSK-J1inhibitsTNF-αproductionbyhumanprimarymacrophagesinanH3K27-dependentmanner[1].GSK-J1inhibitsthedemethylaseactivityofKDM5Cwith8.5-foldincreasedpotencycomparedwiththatofKDM5Bat1mMα-ketoglutarate,withIC50of11μMand94μM,respectively[3].PROTOCOLKinaseAssay[1]PurifiedJmjD3(1μM)andUTX(3μM)isincubatedwith10μMpeptide[BiotinKAPRKQLATKAARK(me3)SAPATGG]in50mMHEPESpH7.5,150mMKCl,50μM(NH4)2SO4·FeSO4·H2O,1mM2-oxoglutarate,and2mMascorbate(JmjD3,3minutesat25°C;UTX,20minutesat25°C)withvariousconcentrationoftheinhibitor(0,0.005,0.01,0.02,0.05,0.1μM).10mMEDTAisaddedtostopthereaction.ThereactionisdesaltedbyziptipandspottedonaMALDIplatewithα-cyano-4-hydroxycinnamicacidMALDImatrix.SamplesareanalysedonaMALDI-TOFRsystem.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•Oncogene.2021Apr;40(15):2711-2724.•ActaPharmacolSin.2021Apr13.•FrontMolNeurosci.2017Mar13;10:51.•JChromatogrA.2020Feb22;1613:460625.•SSRN.2021Dec.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].KruidenierL,etal.AselectivejumonjiH3K27demethylaseinhibitormodulatestheproinflammatorymacrophageresponse.Nature.2012Aug16;488(7411):404-8.[2].HeinemannB,etal.InhibitionofdemethylasesbyGSK-J1/J4.Nature.2014Oct2;514(7520):E1-2[3].HortonJR,etal.CharacterizationofaLinkedJumonjiDomainoftheKDM5/JARID1FamilyofHistoneH3Lysine4Demethylases.JBiolChem.2016Feb5;291(6):2631-46.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidatedfo