SB-202190-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESB202190Cat.No.:HY-10295CASNo.:152121-30-7分?式:C??H??FN?O分?量:331.34作?靶點:p38MAPK;Autophagy;Apoptosis作?通路:MAPK/ERKPathway;Autophagy;Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(301.80mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.0180mL15.0902mL30.1805mL5mM0.6036mL3.0180mL6.0361mL10mM0.3018mL1.5090mL3.0180mL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。-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(jié)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>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(6.28mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.28mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.28mM);ClearsolutionBIOLOGICALACTIVITY?物活性SB202190選擇性的p38MAPK抑制劑，抑制p38α和p38β2的IC50分別為50nM和100nM。SB202190與重組?活性p38激酶的ATP袋結(jié)合，Kd值為38nM。SB202190具有抗癌活性并可以挽救記憶障礙。IC50&Targetp38αp38β250nM(IC50)100nM(IC50)體外研究SB202190(0-10μM;0-72hours)attenuatesgrowthofasubgroupofCRCcelllinessuchasRKO,CACO2andSW480inadose-andtime-dependentmanner[1].SB202190stronglyinhibitedcolonyformationandanchorage-independentgrowth(10μMfor7–10days)andelevatedapoptoticcelldeath(10μMfor72h)inthissamesubsetofCRClines(RKO,CACO2andSW480)[2].InRKO,CACO2andSW480cells,SB202190(10μM;2hours)abrogatesphosphorylationofS6K1(T389)andS6(S235/236),butnotAKT(S473),indicatingthatp38iselectivelyblocksmTORC1signaling[2].體內(nèi)研究SB202190(5mg/kg;intraperitonealinjection;dailyfor10-12days)showsinhibitionoftumorcellsurvivalandtumorgrowth[2].AnimalModel:4-week-oldfemaleBALB/cnudemice(bearingSW480andRKOxenografttumors)[2]Dosage:5mg/kgAdministration:Intraperitonealinjection;dailyfor10-12daysResult:Inhibitionoftumorcellsurvivalandtumorgrowth.戶使?本產(chǎn)品發(fā)表的科研?獻?CellRes.2020Jul;30(7):574-589.?Immunity.19October2022.?EBioMedicine.2015Nov19;2(12):1944-56.?BMCMed.2021Oct15;19(1):247.?CancerLett.2022Jul1;537:215678.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[1].DaviesSP,etal.Specificityandmechanismofactionofsomecommonlyusedproteinkinaseinhibitors.BiochemJ.2000Oct1;351(Pt1):95-105.[2].NemotoS,etal.InductionofapoptosisbySB202190throughinhibitionofp38betamitogen-activatedproteinkinase.JBiolChem.1998Jun26;273(26):16415-20.[3].GrossiV,etal.Bay43-9006inhibitsp38αactivityincolorectalcancercellsandsynergizeswiththeDFG-ininhibitorSB202190toincreaseapoptoticresponse.CancerBiolTher.2012Dec;13(14):1471-81.[4].YangS,etal.Protectiveeffectsofp38MAPKinhibitorSB202190againsthippocampalapoptosisandspatiallearningandmemorydeficitsinaratmodelofvasculardementia.BiomedResInt.2013;2013:215798.[5].ZhangY,etal.PP2ACLevelDeterminesDifferentialProgrammingofp38-TSC-mTORSignalingandTherapeuticResponsetop38-TargetedTherapyinColorectalCancer.EBioMedicine.2015Nov19;2(12):1944-56.McePdfHeightCaution:Productha