Grp94-Inhibitor-1-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGrp94Inhibitor-1Cat.No.:HY-112910CASNo.:2234897-35-7分?式:C??H??N?O?分?量:352.47作?靶點(diǎn):HSP作?通路:CellCycle/DNADamage;MetabolicEnzyme/Protease儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:250mg/mL(709.28mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.8371mL14.1856mL28.3712mL5mM0.5674mL2.8371mL5.6742mL10mM0.2837mL1.4186mL2.8371mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.90mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(5.90mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.90mM);ClearsolutionBIOLOGICALACTIVITY?物活性Grp94Inhibitor-1?種有效的、選擇性的Grp94抑制劑，IC50值為2nM，對(duì)Grp94的抑制作?Hsp90α的1000倍[1]。IC50&TargetGRP942nM(IC50)體外研究Grp94-specificclientsincludeasubsetofintegrinsubunitssuchasintegrinα2andintegrinαL.TheirmaturationandtraffickingtothecellsurfacearedependentontheGrp94chaperonefunctionbuthavenoassociationwithcytoplasmicHsp90α.Grp94Inhibitor-1(1-5μM;36hours)significantlydownregulatedthecellsurfaceexpressionlevelsofintegrinα2andintegrinαLinadose-dependentmannerinpanc1cells[1].WesternBlotAnalysis[1]CellLine:Panc1cellsConcentration:1μM;2.5μM;5μMIncubationTime:36hoursResult:Decreasedintegrinα2andintegrinαLproteinexpression.體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?JVirol.2021Dec1;JVI0110321.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].JiangF,etal.DiscoveryofaPotentGrp94SelectiveInhibitorwithAnti-InflammatoryEfficacyinaMouseModelofUlcerativeColitis.JMedChem.2018Nov8;61(21):9513-9533.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedic