GSK-3β-inhibitor-3-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGSK-3βinhibitor3Cat.No.:HY-141480CASNo.:1448990-73-5分?式:C??H??FNO?S分?量:327.37作?靶點(diǎn):GSK-3;Apoptosis作?通路:PI3K/Akt/mTOR;StemCell/Wnt;Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:250mg/mL(763.66mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.0546mL15.2732mL30.5465mL5mM0.6109mL3.0546mL6.1093mL10mM0.3055mL1.5273mL3.0546mL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(fù)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。-80°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥?式選擇適當(dāng)?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(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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:≥2.08mg/mL(6.35mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.35mM);ClearsolutionBIOLOGICALACTIVITY?物活性GSK-3βinhibitor3?種有效，選擇性，不可逆和共價(jià)的糖原合酶激酶3β(GSK-3β)抑制劑，IC50值為6.6μM。GSK-3βinhibitor3可?于急性早幼粒細(xì)胞??病的研究。IC50&TargetGSK-3β6.6μM(IC50)體外研究GSK-3βinhibitor3(compound4-3)(100μM)inhibitsGSK-3αactivityby87.3%[1].GSK-3βinhibitor3(6.25-100μM;24-48h)dose-dependentlyinhibitsthegrowthofNB4andNB4-R1cells[1].GSK-3βinhibitor3(12.5-100μM;24h)significantlyincreasesthepercentageofapoptosisinadose-dependentpatterninNB4andNB4-R1cells[1].CellViabilityAssay[1]CellLine:NB4andNB4-R1cellsConcentration:6.25,12.5,25,50,100μMIncubationTime:24,48hoursResult:Inhibitedthecellviability,withIC50sof19.56μMand26.42μMinNB4andNB4-R1cellsat24h,respectively.Hadlittlecytotoxicityonhumannormallivercells(LO2)andhumanumbilicalveinendothelialcells(HUVECs).ApoptosisAnalysis[1]CellLine:NB4andNB4-R1cellsConcentration:12.5,25,50,100μMIncubationTime:24hoursResult:Inducedcellapoptosis.體內(nèi)研究GSK-3βinhibitor3(compound4-3)(15mg/kg/d;i.p.for2weeks)inhibitstumorgrowthofmiceby75.97%relativetovehiclecontrol[1].GSK-3βinhibitor3(15mg/kg;asinglei.p.)showslongT1/2of14.2h,highAUCvalues(AUClast=3503.42ng/mL?h),andmaximumconcentration(Cmax=515ng/mL)inmice[1].AnimalModel:Balb/cfemalenudemicewereinjectedleukemiacells[1]2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEDosage:15mg/kg/dAdministration:I.p.for2weeksResult:InhibitedlocalizedgrowthinNB4cells.Hadmildweightlosscomparedwithcontrol.AnimalModel:MaleICRmice(30g)[1]Dosage:15mg/kg(PharmacokineticAnalysis)Administration:Asinglei.p.Result:T1/2=14.2h;AUClast=3503.42ng/mL?h;Cmax=515ng/mL.REFERENCES[1].ZhangP,et,al.DiscoveryofNovelBenzothiazepinonesasIrreversibleCovalentGlycogenSynthaseKinase3βInhibitorsfortheTreatmentofAcutePromyelocyticLeukemia.JMedChem.2021May24.McePdfHeightCaution:Producthasnotbeenfullyvalidated