IU1-47-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEIU1-47Cat.No.:HY-122243CASNo.:670270-31-2分?式:C??H??ClN?O分?量:330.85作?靶點(diǎn):Deubiquitinase作?通路:CellCycle/DNADamage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:16.67mg/mL(50.39mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.0225mL15.1126mL30.2252mL5mM0.6045mL3.0225mL6.0450mL10mM0.3023mL1.5113mL3.0225mL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:≥1.67mg/mL(5.05mM);Clearsolution1/2MasterofBioactiveMolecules—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:≥1.67mg/mL(5.05mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥1.67mg/mL(5.05mM);ClearsolutionBIOLOGICALACTIVITY?物活性IU1-47?種有效的特異性USP14抑制劑，IC50為0.6μM。IU1-47抑制IsoT/USP5，IC50為20μM。IU1-47在培養(yǎng)的神經(jīng)元中誘導(dǎo)tau蛋?降解[1]。IC50&TargetIC50:0.6μM(USP14),20μM(IsoT/USP5)[1]體外研究IU1-47isessentiallyinactiveonfreeUSP14(USP14thatisnotboundtotheproteasome).IU1-47(25μM)antagonizesUSP14deubiquitinatingactivityandstimulatessubstratedegradationinvitro[1].IU1-47stimulatestaudegradationprincipallyviatheubiquitin-proteasomesystem.IU1-47(3μM,10and30μM;48hours)significantlydecreasesTauandphosphotauspeciesSer-202/Thr-205levelsinmurinecorticalprimaryneurons.ThelevelofUSP14itselfdoesnotchange[1].WesternBlotAnalysis[1]CellLine:Murinecorticalprimaryneurons(DIV5)isolatedfromAPPSwe/P301LtransgenicanimalsConcentration:3μM,10and30μMIncubationTime:48hoursResult:SignificantlydecreasedTauandphosphotauspeciesSer-202/Thr-205levels.NochangeinUSP14proteinlevel.REFERENCES[1].BoselliM,etal.AninhibitoroftheproteasomaldeubiquitinatingenzymeUSP14inducestaueliminationinculturedneurons.JBiolChem.2017Nov24;292(47):19209-19225.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch