GSK840-GSK-840-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGSK840Cat.No.:HY-104021CASNo.:2361146-30-5Synonyms:GSK'840分⼦式:C₂₁H₂₃N₃O₃分⼦量:365.43作⽤靶点:RIPkinase作⽤通路:Apoptosis储存⽅式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:110mg/mL(301.02mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.7365mL13.6825mL27.3650mL5mM0.5473mL2.7365mL5.4730mL10mM0.2737mL1.3683mL2.7365mL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>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.75mg/mL(7.53mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.75mg/mL(7.53mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.75mg/mL(7.53mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性GSK840(GSK'840)⼀种受体相互作⽤蛋⽩激酶3(RIP3或RIPK3)抑制剂，⾼亲和⼒结合RIP3激酶结构域，IC50值为0.9nM，并抑制激酶活性，IC50值为0.3nM[1]。IC50&TargetIC50:0.3nM(RIP3)[1]体外研究GSK840(GSK'840)(0.01-3μM;24hours)blocksTNF-inducednecroptosisinaconcentration-dependentmanner[1].GSK840bindsthekinasedomainandinhibitskinaseactivitywithhighspecificity,targetingabroaderrangeofpro-necroticstimulithancanbeachievedwithRIP1kinaseinhibitors[1].CellViabilityAssay[1]CellLine:HumanHT-29cells(TNF10ng/ml+zVAD-fmk20μM+SMAC007100nM)Concentration:0.01-3μMIncubationTime:24hoursResult:BlockedTNF-inducednecroptosisinaconcentration-dependentmanner.户使⽤本产品发表的科研⽂献•CellDeathDiscov.2022Feb26;8(1):88.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].MandalP,etal.RIP3inducesapoptosisindependentofpronecrotickinaseactivity.MolCell.2014Nov20;56(4):481-95.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.