Grp94-Inhibitor-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGrp94Inhibitor-1Cat.No.:HY-112910CASNo.:2234897-35-7分⼦式:C₂₂H₂₈N₂O₂分⼦量:352.47作⽤靶点:HSP作⽤通路:CellCycle/DNADamage;MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(709.28mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.8371mL14.1856mL28.3712mL5mM0.5674mL2.8371mL5.6742mL10mM0.2837mL1.4186mL2.8371mL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:≥2.08mg/mL(5.90mM);Clearsolution1/3MasterofBioactiveMolecules—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:≥2.08mg/mL(5.90mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.90mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Grp94Inhibitor-1⼀种有效的、选择性的Grp94抑制剂，IC50值为2nM，对Grp94的抑制作⽤Hsp90α的1000倍[1]。IC50&TargetGRP942nM(IC50)体外研究Grp94-specificclientsincludeasubsetofintegrinsubunitssuchasintegrinα2andintegrinαL.TheirmaturationandtraffickingtothecellsurfacearedependentontheGrp94chaperonefunctionbuthavenoassociationwithcytoplasmicHsp90α.Grp94Inhibitor-1(1-5μM;36hours)significantlydownregulatedthecellsurfaceexpressionlevelsofintegrinα2andintegrinαLinadose-dependentmannerinpanc1cells[1].WesternBlotAnalysis[1]CellLine:Panc1cellsConcentration:1μM;2.5μM;5μMIncubationTime:36hoursResult:Decreasedintegrinα2andintegrinαLproteinexpression.体内研究Grp94Inhibitor-1(intraperitonealinjection,qid.;coadminbistration10mg/kgor30mg/kg;8days)doesnotattenuatethecolonshortening,butdecreasesdiseaseactivityindex(DAI)scores.ItalsoTNFαandIL-6levelsintheserumandcolonictissuesandsignificantlyreducesthep65expressionincolonictissues,especiallythoseinthe30mg/kgdosegroup[1].AnimalModel:C57BL/6mice(male,20-22g)[1]Dosage:10mg/kgor30mg/kgAdministration:Intraperitonealinjection,qid.;coadminbistration10mg/kgor30mg/kgResult:Decreaseddiseaseactivityindex(DAI)scoresinUCmices.户使⽤本产品发表的科研⽂献•JVirol.2021Dec1;JVI0110321.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].JiangF,etal.DiscoveryofaPotentGrp94SelectiveInhibitorwithAnti-InflammatoryEfficacyinaMouseModelofUlcerativeColitis.JMedChem.2018Nov8;61(21):9513-9533.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedic