KEA1-97-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEKEA1-97Cat.No.:HY-114982CASNo.:2138882-71-8分?式:C??H?Cl?FN?分?量:335.16作?靶點:Caspase;Apoptosis作?通路:Apoptosis儲存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(298.36mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.9836mL14.9182mL29.8365mL5mM0.5967mL2.9836mL5.9673mL10mM0.2984mL1.4918mL2.9836mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(protectfromlight)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.46mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性KEA1-97?種選擇性Thioredoxin-caspase3相互作??擾劑(IC50=10μM)。KEA1-97在不響thioredoxin活性的情況下,破壞thioredoxin與caspase3的相互作?,激活caspases,誘導細胞apoptosis[1]。IC50&TargetCaspase3Thioredoxin10μM(IC50)10μM(IC50)體外研究KEA1-97(100μM;231MFPcells)impairesthioredoxinpulldownofcaspase3[1].KEA1-97(10μM;48hours;231MFPcells)impaires231MFPserum-freecellproliferation[1].KEA1-97(10μM;0~12hours;231MFPcells)activatescaspase3/7andinducesapoptoticcelldeath[1].KEA1-97(231MFPcells)resistantstosurvivalandproliferationimpairments[1].WesternBlotAnalysis[1]CellLine:231MFPcellsConcentration:100μMIncubationTime:Result:Impairedthioredoxinpulldownofcaspase3.CellProliferationAssay[1]CellLine:231MFPcellsConcentration:10μMIncubationTime:48hResult:Impaired231MFPserum-freecellproliferation.ApoptosisAnalysis[1]CellLine:231MFPcellsConcentration:10μMIncubationTime:0~12hResult:Activatedcaspase3/7andinducedapoptoticcelldeath.體內(nèi)研究KEA1-97(5mg/kg;i.p.;50days)attenuatestumorxenograftgrowth[1].AnimalModel:Immune-deficientSCIDmiceDosage:5mg/kg2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEAdministration:I.p.;50daysResult:Attenuatedtumorxenograftgrowth.REFERENCES[1].AndersonKE,etal.Chemoproteomics-EnabledCovalentLigandScreeningRevealsaThioredoxin-Caspase3InteractionDisruptorThatImpairsBreastCancerPathogenicity.ACSChemBiol.2017;12(10):2522-2528.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.For