BD750-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBD750Cat.No.:HY-131140CASNo.:892686-59-8分⼦式:C₁₄H₁₃N₃OS分⼦量:271.34作⽤靶点:JAK;STAT作⽤通路:Epigenetics;JAK/STATSignaling;StemCell/Wnt储存⽅式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(460.68mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.6854mL18.4271mL36.8541mL5mM0.7371mL3.6854mL7.3708mL10mM0.3685mL1.8427mL3.6854mL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>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(7.67mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性BD750⼀个有效的免疫抑制剂，JAK3/STAT5的抑制剂，可抑制IL-2诱导的、JAK3/STAT5依赖的T细胞增殖，其抑制⼩⿏和⼈T细胞增殖的IC50值分别为1.5μM和1.1μM。IC50&TargetJAK3STAT5体外研究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.体内研究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