BAZ2-ICR-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBAZ2-ICRCat.No.:HY-19336CASNo.:1665195-94-7分⼦式:C₂₀H₁₉N₇分⼦量:357.41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DMF:20mg/mL(55.96mM;Needultrasonicandwarming)DMSO:10mg/mL(27.98mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.7979mL13.9895mL27.9791mL5mM0.5596mL2.7979mL5.5958mL10mM0.2798mL1.3990mL2.7979mL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:≥2.5mg/mL(6.99mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.99mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.99mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性BAZ2-ICR⼀种有效的，选择性的，具有细胞活性和⼝服活性的BAZ2A/B溴结构域抑制剂，IC50分别为130nM和180nM，Kd分别为109nM和170nM。BAZ2-ICR结合BAZ2A/B的选择性⽐CECR2⾼10-15倍，⽐其他溴结构域⾼100倍以上。BAZ2-ICR⼀种表观遗传化学探针。IC50&TargetIC50:130nM(BAZ2A)and180nM(BAZ2B);Kd:109nM(BAZ2A)and170nM(BAZ2A)[1]体外研究ToinvestigatewhetherBAZ2-ICR(Compound13)candisplaceBAZ2bromodomainsfromchromatininlivingcells,afluorescencerecoveryafterphotobleaching(FRAP)assayutilizingGFP-taggedBAZ2Afulllengthproteintransfectedintohumanosteosarcomacells(U2OS)aretested.1μMBAZ2-ICRreducestherecoverytimeofthewild-type(wt)constructtoalevelsimilartothedominantnegativemutant,confirmingthatBAZ2-ICRinhibitsBAZ2Aincells[1].体内研究BAZ2-ICR(Compound13)showsveryhighsolubility(25mMinD2O),ameasuredlogDof1.05,highstabilityinmousemicrosomes,andpermeationintheCaCo-2modelandthusasuitableprofilefororalandintravenousgavage.BAZ2-ICR(5mg/kg)shows70%bioavailabilityandmoderateclearance(-50%ofmouseliverbloodflow)andvolumeofdistribution[1].REFERENCES[1].DrouinL,etal.StructureenableddesignofBAZ2-ICR,achemicalprobetargetingthebromodomainsofBAZ2AandBAZ2B.JMedChem.2015Mar12;58(5):2553-9.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Fo