CCG-100602-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECCG-100602Cat.No.:HY-120855CASNo.:1207113-88-9分?式:C??H??ClF?N?O?分?量:478.82作?靶點:Ras作?通路:GPCR/GProtein儲存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(208.85mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.0885mL10.4423mL20.8847mL5mM0.4177mL2.0885mL4.1769mL10mM0.2088mL1.0442mL2.0885mL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；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(protectfromlight)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。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。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥0.83mg/mL(1.73mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥0.83mg/mL(1.73mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性CCG-100602?肌蛋?相關(guān)轉(zhuǎn)錄因?A/?反應因?(MRTF-A/SRF)信號轉(zhuǎn)導的特異性抑制劑。CCG-100602特異性阻斷MRTF-A核定位，從?抑制纖維?成轉(zhuǎn)錄因?SRF[1][2]。體外研究CCG-100602(3-30?μM)decreasesthenumberofadherenthASCcells[2].CCG-100602blockstheexpressionofMRTF-A/SRF-activatedgenes[2].CCG-100602(5-40?μM)diminishestheTGF-β1(5?ng/mL)-inducedincreaseinCOL1A1,FN1,andACTA2transcriptioninadose-dependentmanner[1].CCG-100602(5-40?μM)reducestheTGF-β1-inducedincreaseinMRTFAandSRFmRNAexpressionintheHIMFsinadose-dependentmanner[1].CCG-100602(5-40?μM)significantlyreducestheproteinexpressionlevelsoftheECMandα-SMAinTGF-β1(5?ng/mL)-stimulatedcellsinadose-dependentmanner[1].CCG-100602(5-40?μM)alsosignificantlyrepressestheMRTF-AandSRFproteinexpression,whichwereinducedbyTGF-β1,inthenuclearfractionoftheHIMFsinadose-responsivemanner[1].CellViabilityAssay[2]CellLine:Humanadiposestemcell(hASC)Concentration:3,8,15,or30?μMIncubationTime:7daysResult:Thenumberofadherentcellsdecreasedasaresponsetoincreasinginhibitoramount.Theeffectwasalsodependentontheculturemediabecausetheosteogenicmediumconditionsupportedtheviabilityoverbasicculturemediumandadipogenicmediumconditions.RT-PCR[1]CellLine:Humanintestinalmyofibroblasts(HIMFs)Concentration:5,10,20,and40?μMIncubationTime:30?minpriortotheadditionofTGF-β1(5?ng/mL)for24hoursResult:DiminishedtheTGF-β1-inducedincreaseinCOL1A1,FN1,andACTA2transcriptioninadose-dependentmanner.ReducedtheTGF-β1-inducedincreaseinMRTFAandSRFmRNAexpressionintheHIMFsinadose-dependentmanner.WesternBlotAnalysis[1]CellLine:Humanintestinalmyofibroblasts(HIMFs)Concentration:5,10,20,and40?μM2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEIncubationTime:30?minpriortotheadditionofTGF-β1(5?ng/mL)for48hoursResult:TheproteinexpressionlevelsoftheECMandα-SMAinTGF-β1-stimulatedcellsaresignificantlyreduced.RepressedtheMRTF-Aandserumresponsefactor(SRF)proteinexpression,whichwereinducedbyTGF-β1,inthenuclearfractionoftheHIMFs.體內(nèi)研究TreatmentwithCCG-100602(7.5mg/kg/day,continuouslyadministeredfor2weeksbyosmoticminipumps)abrogatestheincreaseofaorticstiffnessrepresentedbyreducedarterialcomplianceandstrain,indicatingasignificantanti-stiffeningeffectresultingfromtheinhibitionofSRF/myocardin[3].AnimalModel:Adult(4month-old)malespontaneouslyhypertensiverats(SHR)andnormotensivecontrolWistar-Kyoto(WKY)rats[3]Dosage:7.5mg/kg/dayAdministration:Continuouslyadministeredfor2weeksbyosmoticminipumps.Result:Abrogatedtheincreaseofaorticstiffnessrepresentedbyreducedarterialcomplianceandstrain.REFERENCES[1].YoonJeongChoi,etal.Umbilicalcord/placenta-derivedmesenchymalstemcellsinhibitfibrogenicactivationinhumanintestinalmyofibroblastsviainhibitionofmyocardin-relatedtranscriptionfactorA.StemCellResTher.2019Sep23;10(1):291.[2].LauraHyv?ri,etal.Myocardin-RelatedTranscriptionFactorA(MRTF-A)RegulatestheBalancebetweenAdipogenesisandOsteogenesisofHumanAdiposeStemCells.StemCellsInt.2020Sep22;2020:8853541.[3].NingZhou,etal.RhoKinaseRegulatesAorticVascularSmoothMuscleCellStiffnessViaActin/SRF/MyocardininHypertension.CellPhysiolBiochem.201