Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENrf2-IN-1Cat.No.:HY-101025CASNo.:1610022-76-8分?式:C??H??ClN?O?分?量:383.87作?靶點(diǎn):Keap1-Nrf2作?通路:NF-κB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:260mg/mL(677.31mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.6050mL13.0252mL26.0505mL5mM0.5210mL2.6050mL5.2101mL10mM0.2605mL1.3025mL2.6050mL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:≥2.17mg/mL(5.65mM);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:≥2.17mg/mL(5.65mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.17mg/mL(5.65mM);ClearsolutionBIOLOGICALACTIVITY?物活性Nrf2-IN-1Nrf2的抑制劑，被?于急性髓性??病(AML)藥物研究[1]。IC50&TargetNrf2[1]體外研究Nrf2-IN-1(Compound4f)(10μM)inhibitsNrf2activation[1].Nrf2-IN-1(1-20μM;48hours)inhibitsgrowthofthethreeAMLcell[1].Nrf2-IN-1(5-10μM;48hours)inducesapoptosisofthreeAMLcellsinvitro[1].Nrf2-IN-1inducesapoptoticsignalinginvolvingBcl-2andBax[1].CellViabilityAssay[1]CellLine:THP-1cells,HL-60cells,U937cellsConcentration:1μM,5μM,10μM,20μMIncubationTime:48hoursResult:InhibitedgrowthofthethreeAMLcelltypesat5μM,10μMor20μMfor48hours.ApoptosisAnalysis[1]CellLine:THP-1cells,HL-60cells,U937cellsConcentration:5μM,10μMIncubationTime:48hoursResult:InducedapoptosisinAMLcellsinvitro.WesternBlotAnalysis[1]CellLine:THP-1cells,HL-60cells,U937cellsConcentration:5μM,10μMIncubationTime:48hoursResult:Triggeredcaspase-dependentapoptoticsignalinginAMLcells.體內(nèi)研究Nrf2-IN-1inhibitstumorgrowthviaapoptosisinchickeneggs[1].2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?CellsTissuesOrgans.July08,2021.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ZhangJ,etal.DiscoveryofanovelNrf2inhibitorthatinducesapoptosisofhumanacutemyeloidleukemiacells.Oncotarget.2017Jan31;8(5):7625-7636.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.F