Apostatin-1-Apt-1-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEApostatin-1Cat.No.:HY-134050CASNo.:2559703-06-7Synonyms:Apt-1分?式:C??H??N?OS分?量:345.5作?靶點:RIPkinase;Autophagy;Apoptosis;Beclin1;Necroptosis作?通路:Apoptosis;Autophagy儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:83.33mg/mL(241.19mM;ultrasonicandwarmingandadjustpHto4withHClandheatto80°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.8944mL14.4718mL28.9436mL5mM0.5789mL2.8944mL5.7887mL10mM0.2894mL1.4472mL2.8944mL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?。BIOLOGICALACTIVITY?物活性Apostatin-1(Apt-1)?種有效的TRADD抑制劑。Apostatin-1可與TRADD-N結(jié)合(KD=2.17μM)，破壞其與TRADD-C和TRAF2的結(jié)合。Apostatin-1調(diào)節(jié)RIPK1和beclin1的泛素化。Apostatin-1通過激活突變tau、α-synuclein或huntingtin積累的細胞中的?噬(autophagy)，阻斷凋亡(apoptosis)，并恢復細胞內(nèi)穩(wěn)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE態(tài)。體外研究Apostatin-1inhibitsVelcade(Bortezomib,HY-134050)-inducedapoptosisandRIPK1-dependentapoptosis(RDA)andnecroptosis,withanIC50of0.97μM[1].Apostatin-1(10μM,6h)effectivelyinducesautophagyandthedegradationoflong-livedproteins[1].WesternBlotAnalysis[1]CellLine:SH-SY5Y,HeLa,HT-29,andJurkatcellsConcentration:10μMIncubationTime:6hResult:EffectivelyinducedautophagybyLC3IIinductionandp62reduction.體內(nèi)研究Apostatin-1(20mg/kg,IP,once)inhibitsinflammatoryresponses,andincreasessurvivalofsystemicinflammationmousemodel[1].AnimalModel:Wild-typemice(n=10,male,8weeksofage,systemicinflammationmousemodel)[1]Dosage:20mg/kgAdministration:IP,onceResult:ReducedexpressionoftheTNF-inducedinflammatorytargetgeneproducts,NOSandCOXII27,andofinflammatorycytokinesincellsstimulatedwithpathogen-associatedmolecularpatterns,includinginterferonγ(IFNγ),lipopolysaccharide(LPS),Pam3CSK4(asyntheticbacteriallipopeptide),andmuramyldipeptide(MDP).ShowedincreasedsurvivalfollowingintravenousdeliveryofTNF,amousemodelofsystemicinflammation.REFERENCES[1].XuD,etal.ModulatingTRADDtorestorecellularhomeostasisandinhibitapoptosis.Nature.2020Nov;587(7832):133-138.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearc