SSK1-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESSK1Cat.No.:HY-138936CASNo.:2629250-69-5分?式:C??H??F?N?O??分?量:788.61作?靶點:p38MAPK;Apoptosis作?通路:MAPK/ERKPathway;Apoptosis儲存?式:4°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性數(shù)據(jù)體外實驗DMSO:200mg/mL(253.61mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.2681mL6.3403mL12.6805mL5mM0.2536mL1.2681mL2.5361mL10mM0.1268mL0.6340mL1.2681mL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(fù)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(sealedstorage,awayfrommoistureandlight)。-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:≥5mg/mL(6.34mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥5mg/mL(6.34mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性SSK1，?種衰?特異性殺傷化合物，?種β-galactosidase靶向前藥，可減輕炎癥。SSK1被溶酶體β-galactosidase激活，并通過激活p38MAPK和誘導細胞凋亡(apoptosis)選擇性殺死衰?細胞。體外研究SSK1(0.5μM;12-72hours)activatesthephosphorylationlevelsofbothp38MAPKandMKK3/MKK6insenescentcells.SSK1killssenescentcellsthroughtheactivationofthep38MAPKsignalingpathway.SSK1isabletoinducemitochondrialDNAdamageinsenescentcells[1].SSK1(0.01-1μM;3days)selectivelyandpotentlyeliminatesβ-galactosidase-positivesenescentcellswithinawidetherapeuticwindow[1].CellProliferationAssay[1]CellLine:PrimarymousefibroblastsConcentration:0.5?μMIncubationTime:12hours,24hours,36hours,48hours,72hoursResult:Bothp38MAPKandMKK3/MKK6wereactivatedbyphosphorylationinsenescentcells.體內(nèi)研究SSK1(0.5mg/kg;i.p.;twodayseveryweek;forfourweeks)couldeliminatesenescentcellsanddecreasesenescence-associatedmarkersinlung-injuredmice[1].Inagedmice(20-month-old),SSK1(0.5mg/kg;3daysevery2weeksfor8weeks)effectivelyclearssenescentcellsindifferenttissues,decreasesthesenescence-andage-associatedgenesignatures,attenuateslow-gradelocalandsystemicinflammation,andrestoresphysicalfunction[1].AnimalModel:Mice(3-6-month-old)weresubjectedtotranstrachealinjectionofBleomycin[1]Dosage:0.5mg/kgAdministration:Intraperitoneallyinjection;twodayseveryweek;forfourweeksResult:SSK1significantlyreducedthepercentageofSA-β-gal-positivecellsinlungby3.8-foldcomparedwiththatinvehicle-treatedlung-injuredmiceREFERENCES[1].YushengCai,etal.Eliminationofsenescentcellsbyβ-galactosidase-targetedprodrugattenuatesinflammationandrestoresphysicalfunctioninagedmice.CellRes.2020Jul;30(7):574-589.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfor