Fatostatin-125B11-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEFatostatinCat.No.:HY-14452CASNo.:125256-00-0Synonyms:125B11分⼦式:C₁₈H₁₈N₂S分⼦量:294.41作⽤靶点:FattyAcidSynthase(FASN)作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥27mg/mL(91.71mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.3966mL16.9831mL33.9662mL5mM0.6793mL3.3966mL6.7932mL10mM0.3397mL1.6983mL3.3966mL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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。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。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(8.49mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(8.49mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:2.5mg/mL(8.49mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Fatostatin(125B11)SREBP活化的特异性抑制剂，可抑制SREBP-1和SREBP-2的活化。Fatostatin与SCAP(SREBP裂解激活蛋⽩)结合，抑制SREBPs的ER-Golgi易位。Fatostatin降低了细胞中成脂因的转录。Fatostatin具有抗肿瘤作⽤，能降低ob/ob⼩⿏的⾼⾎糖。体外研究Fatostatin(125B11)(0.1-1μM;3days)inhibitstheandrogen-independentprostatecancercellproliferation(IC50=0.1μM)inanindependentoftheknownIGF1-signalingpathway.Fatostatininhibitsinsulin-inducedadipogenesisof3T3-L1cells[1].FatostatindirectlybindsSCAPandblocksitsER-to-GolgitransportwithIC50of2.5and10μMinmammaliancells.CellProliferationAssay[1]CellLine:DU-145cellsConcentration:0.1,1μMIncubationTime:3daysResult:ImpairedtheIGF1-inducedgrowthatanIC50of0.1μM.体内研究Fatostatin(125B11)(30mg/kg;150μL;i.p.injection;dailyfor28days)reducesadiposity,amelioratedfattyliverbyreducingtriglyceride(TG)storage,andloweredhyperglycemiainob/obmice[2].AnimalModel:Four-to-five-week-oldhomozygousmaleobese(ob/ob)mice(C57BL/6J)[2]Dosage:30mg/kg;150μLAdministration:i.p.injection;dailyfor28daysResult:Blockedincreasesinbodyweight,bloodglucose,andhepaticfataccumulationinobeseob/obmice,evenunderuncontrolledfoodintake.户使⽤本产品发表的科研⽂献•CellMetab.2021Aug3;33(8):1655-1670.e8.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•Autophagy.2021Jul;17(7):1592-1613.•JExpClinCancerRes.2019May29;38(1):228.•CellDeathDiffer.2021Jun;28(6):2001-2018.•CellRep.2022Nov29;41(9):111738.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LiXetal.FatostatindisplayshighantitumoractivityinprostatecancerbyblockingSREBP-regulatedmetabolicpathwaysandandrogenreceptorsignaling.MolCancerTher.2014Apr;13(4):855-66.[2].ShaoWetal.FatostatinblocksERexitofSCAPbutinhibitscellgrowthinaSCAP-independentmanner.JLipidRes.2016Aug;57(8):1564-73.[3].InoueKetal.Fatostatin,anSREBPinhibitor,preventedRANKL-inducedbonelossbysuppressionofosteoclastdifferentiation.BiochimBiophysActa.2015Nov;1852(11):2432-41.[4].ChoiY,etal.Identificationofbioactivemoleculesbyadipogenesisprofilingoforganiccompounds.JBiolChem.2003Feb28;278(9):7320-4.[5].KamisukiS,etal.AsmallmoleculethatblocksfatsynthesisbyinhibitingtheactivationofSREBP.ChemBiol.2009Aug28;16(8):882-92.McePdfHeightCaution:Product