Description | SB-431542isapotentandselectiveinhibitorofALK5andALK4withIC50valuesof94nMand14nM,respectivelly,andisalsoaninhibitorofTGF-βReceptor. |
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IC50&Target | IC50:94nM(ALK5),140nM(ALK4) |
InVitro | SB-431542(1μM)significantlyreducestheTGF-β-inducednuclearaccumulationofSmadproteinsinA498cells.SB-431542inhibitsTGF-β1-inducedcollagenIα1andPAI-1mRNAwithIC50valuesof60and50nM,respectively.Inaddition,SB-431542inhibitsTGF-β1-inducedfibronectinmRNAandproteinwithIC50valuesof62and22nM,respectively[1].SB-431542(10μM)isaselectiveinhibitorofendogenousactivinandTGF-βsignalingbuthasnoeffectonBMPsignalinginNIH3T3cells[2].TRKI,SB-431542,inhibitsTGF-beta-inducedtranscription,geneexpression,apoptosis,andgrowthsuppression.SB-431542attenuatesthetumor-promotingeffectsofTGF-beta,includingTGF-beta-inducedEMT,cellmotility,migrationandinvasion,andvascularendothelialgrowthfactorsecretioninhumancancercelllines.SB-431542inducesanchorageindependentgrowthofcellsthataregrowth-inhibitedbyTGF-beta,whereasitreducescolonyformationbycellsthataregrowth-promotedbyTGF-beta[3].SB-431542(0.3μM)inhibitscellproliferationinducedbyTGF-βinMG63cells[4]. |
InVivo | SB-431542(10mg/kg,i.p.)decreaseslungmetastasisbutdoesnotsignificantlyaltergrowthoftheprimarytumor4T1xenograft[5]. |
References |
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PreparingStockSolutions |
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent. | ||||||||||||||||
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KinaseAssay [3] | Atotalof100,000cellsfromeachpoolofA549andHT29areseededintoeachwellof12-wellplate.Cellsareculturedinmediacontaining0.2%FBSfor18hours,andthentreatedwith5ng/mLTGF-β1inthepresenceofSB-431542(10µM)in0.5mLofmediafor24hours.OnehundredμLsofeachsupernatantmediaisusedforVEGFassayaccordingtothemanufacturer"sinstruction.ForTGF-β1ELISA,100,000cellsfromeachpoolofA549,VMRC-LCD,andHT29areseededintoeachwellof12-wellplatesandserum-starvedfor20hours.CellsarethentreatedwithSB-431542in0.5mLofserum-freeRPMImediafor24hours.OnehundredμLsofeachsupernatantmediaisactivatedandusedforTGF-β1assayaccordingtothemanufacturer"sinstruction.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly. | ||||||||||||||||
CellAssay [1] | SB-431542isdissolvedataconcentrationof10mMinDMSO. A498cellsareseededat5,000to10,000cells/wellin96-wellplates.Thecellsareserum-deprivedfor24handthentreatedwithSB-431542for48htoassessthecellulartoxicity.CellviABIlityisdeterminedbyincubatingcellsfor4hwithXTTlabelingandelectroncouplingreagentaccordingtothemanufacturer"sdirections.Livecellswithactivemitochondriaproduceanorange-coloredproduct,formazan,whichisdetectedusingaplatereaderatbetween A 450nm andA 500nm withareferencewavelengthgreaterthan600nm.Theabsorbancevaluescorrelatewiththenumberofviablecells.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly. | ||||||||||||||||
AnimalAdmiNISTration [5] | SB-431542isformulatedin20%DMSO/80%cornoil. Tenthousand4T1cellsareinjectedsubcutaneouslyintothesecondmammaryfatpadof6-week-oldBalb/cfemalemice.Tumorsaremeasuredtwiceweekly,andvolumeiscalculatedusingthefollowingformula:Volume=width2×length×0.52.Micearerandomlyassignedtotwotreatmentgroups:control,n=14(20%DMSO/80%cornoil);SB-431542-treated,n=15(10mg/kgbodyweightin20%DMSO/80%cornoil,administeredintraperitoneallythreetimesperweekstartingonedayaftertumorcellinoculation.Primarytumorsareresectedwhenthevolumeatday10post-injectionof4T1cells.Allmicearemonitoreddailyandeuthanizedafter4weeks.Themetastasesaredissectedtosnap-freezeforfurtheranalysis.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly. | ||||||||||||||||
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MolecularWeight | 384.39 | ||||||||||||
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Formula | C₂₂H₁₆N₄O₃ | ||||||||||||
CASNo. | 301836-41-9 | ||||||||||||
Storage |
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Shipping | RoomtemperatureincontinentalUS;mayvaryelsewhere | ||||||||||||
Solvent&Solubility | DMSO:≥40mg/mL;Ethanol:11.17mg/mL(Needultrasonicandwarming) *"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">1> Purity:99.24%
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