Bisindolylmaleimide-I-hydrochloride-GF109203X-hydrochloride-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBisindolylmaleimideIhydrochlorideCat.No.:HY-13867ACASNo.:176504-36-2Synonyms:GF109203Xhydrochloride;Go6850hydrochloride分⼦式:C₂₅H₂₅ClN₄O₂分⼦量:448.94作⽤靶点:PKC;GSK-3作⽤通路:Epigenetics;TGF-beta/Smad;PI3K/Akt/mTOR;StemCell/Wnt储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:62.5mg/mL(139.22mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2275mL11.1373mL22.2747mL5mM0.4455mL2.2275mL4.4549mL10mM0.2227mL1.1137mL2.2275mL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)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:2.08mg/mL(4.63mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性BisindolylmaleimideI(GF109203X)hydrochloride⼀种具有细胞渗透性和可逆性的PKC抑制剂(对PKCα,PKCβI,PKCβII,andPKCγ的IC50分别为20nM、17nM、16nM和20nM)。BisindolylmaleimideIhydrochloride也⼀种GSK-3抑制剂。IC50&TargetBovinebrainPKCPKC-βIIPKC-βIPKCα10nM(IC50)16nM(IC50)17nM(IC50)20nM(IC50)PKCγFDGFG20nM(IC50)65μM(IC50)体外研究BisindolylmaleimideIhydrochloride(5μM)inhibitsα-thrombin-inducedP47phosphorylation[1].BisindolylmaleimideIhydrochloride(0-1μM)inhibitsDNAsynthesisinquiescentswiss3T3cells[1].BisindolylmaleimideIhydrochloride(5μM)reducesGSK-3activityto25.1±4.3%inadipocyteslysates[3].BisindolylmaleimideIhydrochloride(10μM,24h)inhibitsexosomeandmicrovesicle(EMV)releasefromPC3cells[4].BisindolylmaleimideIhydrochloride(10μM,24h)enhancescytotoxicityof5-fluorouracil(HY-90006)[4].体内研究BisindolylmaleimideIhydrochloride(0.02mg/kg,i.p.)reducedtheinceasedNLRP3,P-PKCɑ,andPKCɑlevelsinmechanicalventilation(MV)group[5].BisindolylmaleimideIhydrochloride(0-20mg/kg,i.p.)reducesthemeanfrequencyofQuinpirole-inducedvomitinginshrews[6].AnimalModel:Quinpirole-treatedshrews[2]Dosage:0-20mg/kgAdministration:i.p.Result:ReducedthemeanfrequencyofQuinpirole-inducedvomiting.BlockedQuinpirole-mediatedERK1/2phosphorylationinshrewbrainstems.户使⽤本产品发表的科研⽂献•JAdvRes.2022Jul13;S2090-1232(22)00156-4.•Theranostics.2021Mar11;11(11):5279-5295.•RedoxBiol.2021Oct;46:102098.•MicrobiolSpectr.2022Aug24;e0105622.•Elife.2021Mar3;10:e60889.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].ToullecD,etal.ThebisindolylmaleimideGF109203XisapotentandselectiveinhibitorofproteinkinaseC.JBiolChem.1991Aug25;266(24):15771-81.[2].VetriF,etal.ImpairmentofneurovascularcouplinginType1DiabetesMellitusinratsispreventedbypancreaticislettransplantationandreversedbyasemi-selectivePKCinhibitor.BrainRes.2017Jan15;1655:48-54.[3].HersI,etal.TheproteinkinaseCinhibitorsbisindolylmaleimideI(GF109203x)andIX(Ro31-8220)arepotentinhibitorsofglycogensynthasekinase-3activity.FEBSLett.1999Nov5;460(3):433-6.[4].KosgodageUS,etal.Chloramidine/Bisindolylmaleimide-I-MediatedInhibitionofExosomeandMicrovesicleReleaseandEnhancedEfficacyofCancerChemotherapy.IntJMolSci.2017May9;18(5):1007.[5].LiuM,etal.Aerobicexercisealleviatesventilator-inducedlunginjurybyinhibitingNLRP3inflammasomeactivation.BMCAnesthesiol.2022Dec1;22(1):369.[6].BelkacemiL,etal.SignaltransductionpathwaysinvolvedindopamineD2receptor-evokedemesisintheleastshrew(Cryptotisparva).AutonNeurosci.2021Jul;233:102807.McePdfHeightC