IN-1130-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEIN-1130Cat.No.:HY-18758CASNo.:868612-83-3分⼦式:C₂₅H₂₀N₆O分⼦量:420.47作⽤靶点:TGF-βReceptor作⽤通路:TGF-beta/Smad储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(237.83mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3783mL11.8915mL23.7829mL5mM0.4757mL2.3783mL4.7566mL10mM0.2378mL1.1891mL2.3783mL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.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥1.43mg/mL(3.40mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性N-1130⼀种⾼度选择性的转化⽣长因⼦-βI型受体激酶(ALK5)抑制剂，对ALK5介导的Smad3磷酸化的IC50为5.3nM。IN-1130抑制酪蛋⽩的ALK5磷酸化(IC50=36nM)，抑制p38α丝裂原活化的蛋⽩激酶(IC50=4.3μM)。IN-1130可抑制阻塞性肾病中的肾纤维化，阻⽌乳腺癌的肺转移。IC50&TargetALK5体外研究IN-1130(0.5,1μM;for2hours)inhibitsTGF-β-stimulatedSmad2phosphorylationandsubsequentnucleartranslocationinHepG2and4T1cells[2].IN-1130(1μM;for72hours)restorestheTGF-β-mediateddecreaseinE-cadherinproteinexpression.IN-1130(1μM;for72hours)inhibitsTGF-β-inducedMMPsmRNAexpressionandthegelatinolyticactivityofsecretedMMPsinMCF10Acells[2].IN-1130(1μM;pretreatedfor30min)inhibitsTGF-β-inducedMDA-MB-231cells,NMuMG,andMCF10Acellsmobilityandinvasion[2].WesternBlotAnalysis[2]CellLine:HepG2and4T1cellsConcentration:0.5,1μMIncubationTime:For2hoursResult:InhibitedTGF-β-stimulatedSmad2phosphorylation.RT-PCR[2]CellLine:MCF10AcellsConcentration:1μMIncubationTime:For72hoursResult:InhibitedTGF-β-inducedMMPsmRNAexpressionandthegelatinolyticactivityofsecretedMMPs.体内研究IN-1130(10,20mg/kg/day;IP;for7and14days)reducestheextentofinterstitialnephritisandfibrosis(arrowheads)with10mg/kgandsignificantlyreducesorabsenthistopathologicalchangeswith20mg/kginunilateralureteralobstruction(UUO)rats[1].IN-1130(10,20mg/kg/day;for14days)dose-dependentlydecreaseslevelsofTGF-β1mRNAandsuppressesphosphorylationofSmad2,α-SMA,myofibroblastsinratUUOkidneys[1].IN-1130(40mg/kg;IP;3timesperweekfor3weeks)inhibitsinvivobreastcancermetastasistothelungsinMMTV/c-Neumice(Eight-week-oldfemaleBALB/cmice)[2].2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:Six-week-oldmaleSprague–Dawleyratsweighing180-200g[1]Dosage:10and20mg/kgAdministration:IP;daily;for7and14daysResult:Reducedtheextentofinterstitialnephritisandfibrosis(arrowheads)with10mg/kg.REFERENCES[1].MoonJA,etal.IN-1130,anoveltransforminggrowthfactor-betatypeIreceptorkinase(ALK5)inhibitor,suppressesrenalfibrosisinobstructivenephropathy.KidneyInt.2006Oct;70(7):1234-43.[2].ParkCY,etal.AnnovelinhibitorofTGF-βtypeIreceptor,IN-1130,blocksbreastcancerlungmetastasisthroughinhibitionofepithelial-mesenchymaltransition.CancerLett.2014Aug28;351(1):72-80.McePdfHeightCaution:Producthasnotbeenf