CeMMEC13-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECeMMEC13Cat.No.:HY-101088CASNo.:1790895-25-8分⼦式:C₁₉H₁₆N₂O₄分⼦量:336.34作⽤靶点:DNA/RNASynthesis作⽤通路:CellCycle/DNADamage储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥30mg/mL(89.20mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.9732mL14.8659mL29.7318mL5mM0.5946mL2.9732mL5.9464mL10mM0.2973mL1.4866mL2.9732mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(7.43mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.43mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.43mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性CeMMEC13⼀种有效的TAF1(2)抑制剂，IC50值为2.1μM。IC50&TargetIC50:2.1μM(TAF1(2))[1]体外研究CeMMEC13isapotentinhibitorofTAF1(2)bromodomain,withanIC50of2.1μM.CeMMEC13showslittleornoeffectsonREDNESS,BRD4,CREBBP.CeMMEC13(0-20μM)incombinationwith(S)-JQ1increasesRFPexpressioninREDS3cellsandiseffectivereducingtheviabilityofH23andTHP1cells,betterthanthatofsingletreatment[1].PROTOCOLKinaseAssay[1]TAF1bindingassaysareconductedusingtheEPIgeneousBindingDomainkitB.BindingisdeterminedbythedisplacementofanacetylatedbiotinpeptidefromaGST-taggedTAF1proteinusingHTRFwithaEu3+-conjugatedGSTantibodydonorandstreptavidin-conjugatedacceptor.Compounds(CeMMEC13)aredispensedintoassayplates,ProxiPlate-384PlususinganEcho525LiquidHandler.Bindingassaysareconductedinafinalvolumeof20μLwith5nMTAF1-GST,50nMpeptide(SGRGK(ac)GGK(ac)GLGK(ac)GGAK(ac)RHRK(biotin)-acid),6.25nMStreptavidin-XL665,1:200Anti-GST-Eu3+cryptateand0.1%DMSO.AssayreagentsaredispensedintoplatesusingaMultidropcombiandincubatedatroomtemperaturefor3h.FluorescenceismeasuredusingaPHERAstarmicroplatereaderusingtheHTRFmodulewithdualemissionprotocol(A=excitationof320nm,emmissionof665nm,andB=excitationof320nm,emissionof620nm).RawdataareprocessedtogiveanHTRFratio(channelA/B×10,000),whichisusedtogenerateIC50curves[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.CellAssay[1]Cellsareseededonclearflat-bottom96-wellor384-wellplatesandtreatedwiththeindicatedcompounds(CeMMEC13)forthespecifiedconditions.Live-cellimagingpicturesaretakenwiththeOperettaHighContentScreeningSystem,20×objectiveandnonconfocalmode[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•BiochemPharmacol.2021Feb1;185:114435.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].SdelciS,etal.MappingthechemicalchromatinreactivationlandscapeidentifiesBRD4-TAF1cross-talk.NatChemBiol.2016Jul;12(7):504-10.McePdfHeightCaution:Producthasnot