SKI-V-DataSheet-生命科學試劑-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemESKIVCat.No.:HY-12895CASNo.:24418-86-8分?式:C??H??O?分?量:254.24作?靶點:SPHK;PI3K;Apoptosis作?通路:Immunology/Inflammation;PI3K/Akt/mTOR;Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:250mg/mL(983.32mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.9333mL19.6665mL39.3329mL5mM0.7867mL3.9333mL7.8666mL10mM0.3933mL1.9666mL3.9333mL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，并請注意儲備液的保存?式和期限。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，配制前請先配制澄的儲備液，再依次添加助溶劑(為保證實驗結(jié)果的可靠性，體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；澄的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分?指該溶劑在您配制終溶液中的體積占?)：1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(8.18mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(8.18mM);ClearsolutionBIOLOGICALACTIVITY1/3MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemE?物活性SKIV?種?競爭性的，有效的?脂質(zhì)鞘氨醇激酶(SPHK;SK)抑制劑，對GST-hSK的IC50為2μM。SKIV有效抑制PI3K，對hPI3k的IC50為6μM。SKIV減少有絲分裂的第?信使鞘氨醇-1-磷酸(S1P)的形成。SKIV誘導細胞凋亡(apoptosis)并具有抗腫瘤活性。IC50&TargetIC50:2μM(GST-hSK),6μM(hPI3k)and80μM(ERK2)[1]體外研究SKIVhasweakactivitytowardERK2(IC50of80μMforhERK2)anddoesnotinhibitPKC-α[1].SKIV(10μM;for24hours)inhibitscancercellproliferationandinducesapoptosis[1].SKIV(0.2,1,5μM;pretreatedfor1hour)decreasesphospho-Aktandphospho-MEKlevels.Near-confluentculturesofJCcellsareserum-starvedfor16hours,followedbypretreatmentSKIVfor1hour[2].SKIVhasIC50sforinhibitionofsphingosinekinase(SK)andtumorcellproliferationof-2μM[1].SKIV(20μg/ml)inhibitsnotonlypurifiedbutendogenousSKininMDA-MB-231cells[1].SKIV(0.2,1,5μM)inhibitsintracellularS1PformationinJCcellsinadose-dependentfashion[2].CellProliferationAssay[1]CellLine:T24tumorcellsConcentration:10μMIncubationTime:For24hoursResult:Inhibitedcancercellproliferation.ApoptosisAnalysis[1]CellLine:T24tumorcellsConcentration:10μMIncubationTime:For24hoursResult:Inducedapoptosis.WesternBlotAnalysis[2]CellLine:JCcellsConcentration:0.2,1,5μMIncubationTime:Pretreatedfor1hourResult:Decreasedphospho-Aktandphospho-MEKlevels.體內(nèi)研究SKIV(75mg/kg;i.p.;days1,5,9,15)significantlylowerstumorgrowth(>50%decreasedatday18)thancontrolanimals[1].AnimalModel:6-8weeksoldBALB/cfemalemicewithJCmammaryadenocarcinomacells[1]2/3MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemEDosage:75mg/kgAdministration:IP;days1,5,9,15Result:Tumorgrowthwassignificantlylower(>50%decreasedatday18)thantumorgrowthincontrolanimals.REFERENCES[1].FrenchKJ,etal.Discoveryandevaluationofinhibitorsofhumansphingosinekinase.CancerRes.2003Sep15;63(18):5962-9.[2].FrenchKJ,etal.Antitumoractivityofsphingosinekinaseinhibitors.JPharmacolExpTher.2006Aug;318(2):596-603.McePdfHeightCaution:Producthasnotbeenfullyvalidate