SKI-V-DataSheet-生命科学试剂-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemESKIVCat.No.:HY-12895CASNo.:24418-86-8分⼦式:C₁₅H₁₀O₄分⼦量:254.24作⽤靶点:SPHK;PI3K;Apoptosis作⽤通路:Immunology/Inflammation;PI3K/Akt/mTOR;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(983.32mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.9333mL19.6665mL39.3329mL5mM0.7867mL3.9333mL7.8666mL10mM0.3933mL1.9666mL3.9333mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存⽅式和期限。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(8.18mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(8.18mM);ClearsolutionBIOLOGICALACTIVITY1/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE⽣物活性SKIV⼀种⾮竞争性的，有效的⾮脂质鞘氨醇激酶(SPHK;SK)抑制剂，对GST-hSK的IC50为2μM。SKIV有效抑制PI3K，对hPI3k的IC50为6μM。SKIV减少有丝分裂的第⼆信使鞘氨醇-1-磷酸(S1P)的形成。SKIV诱导细胞凋亡(apoptosis)并具有抗肿瘤活性。IC50&TargetIC50:2μM(GST-hSK),6μM(hPI3k)and80μM(ERK2)[1]体外研究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.体内研究SKIV(75mg/kg;i.p.;days1,5,9,15)significantlylowerstumorgrowth(>50%decreasedatday18)thancontrolanimals[1].AnimalModel:6-8weeksoldBALB/cfemalemicewithJCmammaryadenocarcinomacells[1]2/3MasterofSmallMolecules—您⾝边的抑制剂⼤师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