Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECeMMEC13Cat.No.:HY-101088CASNo.:1790895-25-8分?式:C??H??N?O?分?量:336.34作?靶點(diǎn):DNA/RNASynthesis作?通路:CellCycle/DNADamage儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥30mg/mL(89.20mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.9732mL14.8659mL29.7318mL5mM0.5946mL2.9732mL5.9464mL10mM0.2973mL1.4866mL2.9732mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請?jiān)?個?內(nèi)使?，-20°C儲存時，請?jiān)?個?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(7.43mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.43mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.43mM);ClearsolutionBIOLOGICALACTIVITY?物活性CeMMEC13?種有效的TAF1(2)抑制劑，IC50值為2.1μM。IC50&TargetIC50:2.1μM(TAF1(2))[1]體外研究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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?BiochemPharmacol.2021Feb1;185:114435.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEREFERENCES[1].SdelciS,etal.MappingthechemicalchromatinreactivationlandscapeidentifiesBRD4-TAF1cross-talk.NatChemBiol.2016Jul;12(7):504-10.McePdfHeightCaution:Producthasnot