BRD3308-DataSheet-生命科学试剂-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEBRD3308Cat.No.:HY-19618CASNo.:1550053-02-5分⼦式:C₁₅H₁₄FN₃O₂分⼦量:287.29作⽤靶点:HDAC;HIV作⽤通路:CellCycle/DNADamage;Epigenetics;Anti-infection储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(870.20mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.4808mL17.4040mL34.8080mL5mM0.6962mL3.4808mL6.9616mL10mM0.3481mL1.7404mL3.4808mL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，并请注意储备液的保存⽅式和期限。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，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(7.24mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(7.24mM);ClearsolutionBIOLOGICALACTIVITY1/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE⽣物活性BRD3308⼀种⾼选择性的HDAC3抑制剂，IC50为54nM。BRD3308对HDAC3的选择性HDAC1(IC50为1.26μM)或HDAC2(IC50为1.34μM)的23倍。BRD3308抑制由炎性细胞因⼦或糖脂毒性应激诱导的胰腺β细胞凋亡，并增加功能性胰岛素释放。BRD3308还可激活HIV-1转录并破坏HIV-1潜伏期。IC50&TargetHDAC3HDAC3HDAC1HDAC154nM(IC50)29nM(Ki)1260nM(IC50)5100nM(Ki)HDAC2HDAC2HIV-11340nM(IC50)6300nM(Ki)体外研究BRD3308(5-30µM;6-24hours)treatmentincreasesHIV-1expressioninthe2D10cellline[1].BRD3308(15µM;overnight)isabletoinduceoutgrowthofHIV-1fromlatentlyinfectedcellsexvivoinrestingCD4+Tcells[1].BRD3308inhibitsHDAC1,HDAC2andHDAC3withKivaluesof5.1μM,6.3μMand29nM,respectively[3].RT-PCR[1]CellLine:2D10cellsConcentration:5µM,10µM,15µM,or30µMIncubationTime:6hours,12hours,18hours,or24hoursResult:AnincreaseinHIV-1expressionwasobserved.体内研究BRD3308(5mg/kg;intraperitonealinjection;everysecondday;maleZuckerDiabeticFattyrats)treatmentreduceshyperglycaemiaandincreasesinsulinsecretioninaratmodeloftype2diabetes.Attheendofthehyperglycaemicclamp,circulatinginsulinlevelsaresignificantlyhigherinBRD3308-treatedrats.Pancreaticinsulinstainingandcontentsarealsosignificantlyhigher.BRD3308preservesthefunctionalβ-cellmassagainstglucolipotoxicityinvivo[2].AnimalModel:MaleZuckerDiabeticFatty(Obese)rats(6-week-old)[2]Dosage:5mg/kgAdministration:Intraperitonealinjection;everyseconddayResult:Reducedhyperglycaemiaandincreasedinsulinsecretioninaratmodeloftype2diabetes.REFERENCES[1].BartonKM,etal.SelectiveHDACinhibitionforthedisruptionoflatentHIV-1infection.PLoSOne.2014Aug19;9(8):e102684.[2].LundhM,etal.Histonedeacetylase3inhibitionimprovesglycaemiaandinsulinsecretioninobesediabeticrats.DiabetesObesMetab.2015Jul;17(7):703-7.2/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE[3].WagnerFF,etal.AnIsochemogenicSetofInhibitorsToDefinetheTherapeuticPotentialofHistoneDeacetylasesinβ-CellProtection.ACSChemBiol.2016Feb19;11(2):363-74.McePdfHeightCaution:Producthasnotbeenfullyvalidat