I-BRD9-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEI-BRD9Cat.No.:HY-18975CASNo.:1714146-59-4分⼦式:C₂₂H₂₂F₃N₃O₃S₂分⼦量:497.55作⽤靶点:EpigeneticReaderDomain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:13.89mg/mL(27.92mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0098mL10.0492mL20.0985mL5mM0.4020mL2.0098mL4.0197mL10mM0.2010mL1.0049mL2.0098mL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:≥1.39mg/mL(2.79mM);Clearsolution1/2MasterofBioactiveMolecules—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:≥1.39mg/mL(2.79mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥1.39mg/mL(2.79mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性I-BRD9含溴结构域蛋⽩9(BRD9)的选择性细胞化学探针，其pIC50值为7.3μM。I-BRD9对溴结构域和额外末端结构域(BET)家族和⾼度同的含溴结构域蛋⽩7(BRD7)具有很⾼的选择性。I-BRD9可⽤于识别Kasumi-1细胞中受BRD9调控的参与肿瘤和免疫应答通路的因。体外研究I-BRD9(10μM,6h)hasaregulationroleincancerandimmunologypathways[1].I-BRD9(10μM)hashighBRD9affinityandexcellentbroaderbromodomainselectivity[1].I-BRD9(10μM)hasaffinityforBRD9(TR-FRET),BRD4BD1(TR-FRET)andBRD9NanoBRETwithpIC50valuesof7.3μM,5.3μMand6.8μM[1].I-BRD9(10μM)hashighaqueoussolubility(CLND)with359μM[1].I-BRD9(10μM)displays>625foldselectivityinbindingwithendogenousBRD9againstBETfamilymemberBRD3inHUT-78celllysate[1].RT-PCR[1]CellLine:Kasumi-1cellsConcentration:10μMIncubationTime:6hResult:Showed4genes(CLEC1,62DUSP6,63FES64andSAMSN165)thatwerestronglydown-regulatedandnotbyI-BET151.户使⽤本产品发表的科研⽂献•ProcNatlAcadSciUSA.2019Feb19;116(8):2961-2966.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].NatalieHTheodoulou,etal.DiscoveryofI-BRD9,aSelectiveCellActiveChemicalProbeforBromodomainContainingProtein9Inhibition.JMedChemMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresear