Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBD750Cat.No.:HY-131140CASNo.:892686-59-8分?式:C??H??N?OS分?量:271.34作?靶點:JAK;STAT作?通路:Epigenetics;JAK/STATSignaling;StemCell/Wnt儲存?式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:125mg/mL(460.68mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.6854mL18.4271mL36.8541mL5mM0.7371mL3.6854mL7.3708mL10mM0.3685mL1.8427mL3.6854mL請根據(jù)產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，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據(jù)您的實驗動物和給藥?式選擇適當?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：(為保證實驗結果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(7.67mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性BD750?個有效的免疫抑制劑，JAK3/STAT5的抑制劑，可抑制IL-2誘導的、JAK3/STAT5依賴的T細胞增殖，其抑制??和?T細胞增殖的IC50值分別為1.5μM和1.1μM。IC50&TargetJAK3STAT5體外研究BD750inhibitshumanTcellproliferationstimulatedeitherbyanti-CD3/anti-CD28mAbsorbyalloantigeninadose-dependentmannerwithIC50valuesof1.1±0.2μMand1.3±0.2μMrespectively[1].BD750alsoinhibitsConA,PMA/ionomycineoralloantigen-inducedmouseTcellproliferationandPHAorPMA/ionomycine-inducedhumanTcellproliferation[1].BD750(5or20μM)inhibitstheLPS-inducedJAK-STAT5signalinginDC[2].WesternBlotAnalysis[2]CellLine:PurifiedimmatureDCs.Concentration:1,5or20μM.IncubationTime:12h.Result:HadfewersmalldendritesandsmallerclustersthantypicalmDCs(5or20μM).AtahigherdosesignificantlyreducedthelevelsofLPS-stimulatedIL-6,IL-12,TNF-α,IL-1βandIL-23productionbyDCs.體內研究BD750caninducetolerogenicdendriticcells(tolDC)andtheirfunctioninexperimentalautoimmuneencephalitis(EAE)inmice[2].AnimalModel:FemaleC57BL/6mice(10wksold,19-21g)[2].Dosage:20μM.Administration:IV,treatedDCond7,11and15postthefirstPTXinjection(dpi7,11and15).Result:SignificantlyreducedthefrequencyofTh1andTh17cellsandincreasedthepercentageofTregscomparedwithmicereceivingPBS.REFERENCES[1].YLiu,etal.BD750,abenzothiazolederivative,inhibitsTcellproliferationbyaffectingtheJAK3/STAT5signallingpathway.BrJPharmacol.2013Feb;168(3):632-43.[2].YanZhou,etal.TolerogenicdendriticcellsinducedbyBD750ameliorateproinflammatoryTcellresponsesandexperimentalautoimmuneencephalitisinmice.MolMed.2017Oct;23:204-214.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplic