KDM5-IN-1-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEKDM5-IN-1Cat.No.:HY-100422CASNo.:1628210-26-3分?式:C??H??N?O分?量:324.38作?靶點(diǎn):HistoneDemethylase作?通路:Epigenetics儲(chǔ)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(92.48mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.0828mL15.4140mL30.8280mL5mM0.6166mL3.0828mL6.1656mL10mM0.3083mL1.5414mL3.0828mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)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(chǔ)備液可以根據(jù)儲(chǔ)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(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(6.41mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.41mM);Clearsolution3.請(qǐng)依序添加每種溶劑：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.5mg/mL(7.71mM);ClearsolutionBIOLOGICALACTIVITY?物活性KDM5-IN-1?效選擇，有?服活性的KDM5抑制劑，IC50值為15.1nM。IC50&TargetIC50:15.1nM(KDM5);EC50:0.34μM(PC9H3K4Me3)[1]體外研究KDM5-IN-1isfoundtopotentlyinhibitKDM5BandKDM5Cisoforms(IC50of4.7and65.5nM,respectively).ItissignificantlylesspotentagainstotherKDMenzymes(1A,2B,3B,4C,5A,6A,7B),inhibitingKDM4CthestrongestwithanIC50of1.9μM.KDM5-IN-1stilldisplaysmorethan100-foldselectivityforKDM4Cvs.KDM5A[1].體內(nèi)研究Whendosedorallyinmiceat50mg/kgtwiceaday,KDM5-IN-1showsanunboundmaximalplasmaconcentrationCmax>15-foldoveritscellEC50,therebyprovidingarobustchemicalprobeforstudyingKDM5biologicalfunctionsinvivo[1].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?ActaPharmacolSin.2021Apr13.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LiangJ,etal.Leadoptimizationofapyrazolo[1,5-a]pyrimidin-7(4H)-onescaffoldtoidentifypotent,selectiveandorallybioavailableKDM5inhibitorssuitableforinvivobiologicalstudies.BioorgMedChemLett.2016Aug15;26(16):4036-41.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch