Spautin-1-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESpautin-1Cat.No.:HY-12990CASNo.:1262888-28-7分?式:C??H??F?N?分?量:271.26作?靶點(diǎn):Autophagy;Apoptosis作?通路:Autophagy;Apoptosis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:50mg/mL(184.32mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.6865mL18.4325mL36.8650mL5mM0.7373mL3.6865mL7.3730mL10mM0.3687mL1.8433mL3.6865mL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(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(9.22mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(9.22mM);ClearsolutionBIOLOGICALACTIVITY?物活性Spautin-1?種特異性和有效的?噬抑制劑，可抑制泛素特異性肽酶USP10和USP13，IC50s約為0.6-0.7μM。體外研究Spautin-1enhancesimatinibmesylate(IM)-inducedCmLcellapoptosisbyreducingtheexpressionoftheanti-apoptoticproteinsMcl-1andBcl-2.Thepro-apoptoticactivityofspautin-1isassociatedwithactivationofGSK3β,animportantdownstreameffectorofPI3K/AKT.Spautin-1enhancesIM-inducedcytotoxicityinCmLcelllineK562,decreasingtheIC50from1to0.5μM[1].Themechanismofspautin-1actingonacutepancreatitisisassociatedwithimpairedautophagyinhibition[2].體內(nèi)研究Spautin-1amelioratesthepathogenesisofacutepancreatitisinducedbyceruleinorL-arginine.Spautin-1pretreatmentsignificantlydiminishestheelevationofserumamylaseandlipaselevels,whichareindicativeoftrypsinactivity.IncreasinglevelsofserumTNFαcausedbyceruleinareinhibitedinthepresenceofspautin-1.Spautin-1treatmentcanamelioratetheinflammationdamageinducedbycerulein,suchasedema,degeneration,coagulativenecrosisandinfiltrationofinflammatorycells[2].PROTOCOLCellAssay[1]Spautin-1isdissolvedinDMSO.CellproliferationisevaluatedusingCCK-8kit.K562cells(1x105/mL)areseededinto96-wellplatesintriplicateandthentreatedwith125to4,000nMIMaloneorincombi?nationwithspautin-1(10μM).After48hofincubation,10μLofCCK-8reagentisaddedtoeachwell.Fourhourslater,theabsorbanceisreadat450nmusingamicroplatereader[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice:Inthisstudy,micemodelswithacutepancreatitis,includingcerulein-andL-arginine-inducedmodels,Administration[2]areconstructed.Forthecerulein-inducedmodel,fourintraperitonealinjectionsofcerulein(50μg/kgbodyweight)aregivenconsecutivelyathourlyintervals;TheL-arginine-inducedmodelreceivedhourlyintraperitonealinjectionsof1.4g/kg(optimaldosageforthisstudy)L-argininethreetimes[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?NatCommun.2022Mar31;13(1):1700.?JCellMolMed.2021May2.?ResearchSquarePrint.September14th,2022.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEREFERENCES[1].ShaoS,etal.Spautin-1,anovelautophagyinhibitor,enhancesimatinib-inducedapoptosisinchronicmyeloidleukemia.IntJOncol.2014May;44(5):1661-1668.[2].XiaoJ,etal.Spautin-1AmelioratesAcutePancreatitisviaInhibitingImpairedAutophagyandAlleviatingCalciumOverload.MolMed.2016Aug18;22.McePdfHeightCaution:Pr