NSC-23766-trihydrochloride-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENSC23766trihydrochlorideCat.No.:HY-15723ACASNo.:1177865-17-6分?式:C??H??Cl?N?分?量:530.96作?靶點:Ras;Apoptosis作?通路:GPCR/GProtein;Apoptosis儲存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實驗DMSO:33.33mg/mL(62.77mM;Needultrasonic)H2O:≥32mg/mL(60.27mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.8834mL9.4169mL18.8338mL5mM0.3767mL1.8834mL3.7668mL10mM0.1883mL0.9417mL1.8834mL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(sealedstorage,awayfrommoisture)。-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>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(4.71mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.71mM);Clearsolution3.請依序添加每種溶劑：PBSSolubility:110mg/mL(207.17mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性NSC23766trihydrochlorideRac1激活的抑制劑。體外研究NSC23766(100?μM)treatmenteffectivelyinhibitspolarbodyemissioninadose-dependentmanner.NSC23766(200μM)increasesthepercentageofmorphologicallyabnormalspindlesofoocytes.InNSC23766-treatedoocytes,thep-MAPKproteinexpressionissignificantlydecreased[2].NSC23766(50?μM)plus100?ng/mLJagged1,GDF9andBMP15,reducesthenumberofgermLinecellcystsandincreasesthenumberofprimordialfollicles[3].NSC23766significantlyinhibitsGTP-Rac1activityandphosphorylationofRac1-PAK,ERKsandp38MAPKinthespinaldorsalhornneurons[4].體內(nèi)研究NSC23766(2.5mg/kg/day,i.p.)significantlyattenuatestheonsetofspontaneousdiabetesinNODmice,withoutsignificanteffectsonthegrowth(bodyweights)ofthemice.NSC23766significantlyincreasestheexpressionofRac1andCHOP,amarkerforER-stress,inisletsfromNODmice[1].PROTOCOLKinaseAssay[4]Briefly,freshspinalcordtissueofthelumbarenlargementishomogenisedinthepresenceofproteaseandphosphataseinhibitorsandlysedwithbuffer.Afterbeingcentrifugedat12,000×gfor5minat4°C,thesupernatantsarecollectedandincubatedwithPAK-PBDbeadsat4°Conarotatorfor1handthenthebeadsarepelletedthroughcentrifugationat5000×gfor3minat4°C.TheresultingpelletisresuspendedinLaemmLibufferandboiledfor2min.ThebeadsamplesaresubjectedtoWesternblotanalysis.TotalRac1ineachsampleisalsodeterminedbyWesternblotanalysis.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalBalb/ccontrolandNODmiceareat7weeksofageandaredividedintofourgroups(n=8/group).At8weeksAdministration[1]ofagetwogroupsofexperimentalanimals(Balb/candNOD)receiveNSC23766(2.5mg/kg/day,i.p./daily)andothertwogroups,whichserveascontrolBalb/candNODmiceandreceiveequalvolumeofsaline.Thebodyweightsandbloodglucosearemonitoredeveryweekfor34weeks.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻?AdvSci(Weinh).2021Mar8;8(10):2004000.?BioactMater.2021Jun1.?CellDeathDis.2022Feb17;13(2):158.?FrontImmunol.2021Aug2;12:686846.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE?FrontImmunol.02August2021.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].VeluthakalR,etal.NSC23766,aKnownInhibitorofTiam1-Rac1SignalingModule,PreventstheOnsetofType1DiabetesintheNODMouseModel.CellPhysiolBiochem.2016;39(2):760-7.[2].SongSJ,etal.InhibitionofRac1GTPaseactivityaffectsporcineoocytematurationandearlyembryodevelopment.SciRep.2016Oct3;6:34415[3].ZhaoL,etal.Rac1modulatestheformationofprimordialfolliclesbyfacilitatingSTAT3-directedJagged1,GDF9andBMP15transcriptioninmice.SciRep.2016Apr6;6:23972[4].WangY,etal.InvolvementofRac1signallingpathwayinthedevelopmentandmaintenanceofacuteinflammatorypaininducedbybeevenominjection.BrJPharmacol.2016Mar;