GSTO1-IN-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGSTO1-IN-1Cat.No.:HY-111530CASNo.:568544-03-6分⼦式:C₁₀H₁₂Cl₂N₂O₃S分⼦量:311.18作⽤靶点:GutathioneS-transferase作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥300mg/mL(964.07mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.2136mL16.0679mL32.1357mL5mM0.6427mL3.2136mL6.4271mL10mM0.3214mL1.6068mL3.2136mL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>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(8.03mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(8.03mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(8.03mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性GSTO1-IN-1⼀种有效的⾕胱⽢肽S-转移酶omega1(GSTO1)抑制剂，IC50为31nM。IC50&TargetIC50:31nM(GSTO1)[1]体外研究GSTO1-IN-1(C1-27)potentlyinhibitsGSTO1enzymeactivitywithanIC50valueof31nM.GSTO1-IN-1alsopotentlycompeteswith5-chloromethylfluoresceindiacetate(CMFDA)forbindingtorecombinantprotein,aswellasendogenousGSTO1inthemilieuofasolubleproteome.HCT116cellstreatedwithGSTO1-IN-1alsoshowadecreaseincellviabilityinadose-dependentmanner.GSTO1-IN-1inhibitstheclonogenicsurvivalofHCT116cellsatsub-micromolarconcentrations[1].体内研究TotestwhetherGSTO1-IN-1hadinvivoefficacy,itseffectsareevaluatedinahumancoloncancercelllinexenograftmodel.GSTO1-IN-1(20-45mg/kg)isadministeredasasingleagenttonudemicebearingHCT116xenografts.After5weeksoftreatment,tumorgrowthissignificantlyinhibitedinGSTO1-IN-1-treatedmicecomparedwiththevehicle-treatedgroup(P[1].PROTOCOLCellAssay[1]CellproliferationisassessedbyaMTTassay.CancercellsH630,HT29andHCT116areseededin96-wellmicrotitreplatesand,afterovernightattachment,treatedwithGSTO1inhibitors(e.g.,GSTO1-IN-1;0.1,1,10and100μM).After72h,MTTsolution(3mg/mL;20mL)isaddedtoeachwellandcellsareincubatedfor3hat37°C.Afterincubation,mediafromeachwellisremovedandthedarkblueformazancrystalsformedbylivecellsaredissolvedinDMSO(150mLperwell).Theabsorbanceintensityismeasuredat570nmonamicroplatereader.Cellviabilityafter24htreatmentisassessedusingApoTox-Glotriplexassay.Atleastthreeindependentdose-responseexperimentswitheachconcentrationtestedintriplicateareperformedforeachcellline[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice[1]Administration[1]Inthepilotstudy,HCT116cells(1×106)inexponentialphaseareinjectedsubcutaneouslyintotheleftflankof8-to10-week-oldfemalenudemice(25-30g).Theperpendiculardiametersofthetumorsaremeasuredthreetimesweeklyusingstandardcalipersandtumourvolumesarecalculated.Tumorsareallowedtogrowtoavolumeof50mm3andmicearerandomizedintocontrol(n=5)andGSTO1-IN-1(n=3)treatmentgroups.GSTO1-IN-1isadministeredintraperitoneally(20mg/kgperday)forthefirst2weeksona5dayson/2daysoffschedule.Thedoseisthenincreasedto25mg/kgperdayforthenext23daysandfurtherescalatedby52/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEmg/kgperdaytoafinaldoseof45mg/kgfortheremainingdurationoftreatment.Tumorvolumesandbodyweightsaremeasuredthreetimesweeklytomonitortumorburdenandweightlossduringtreatment.Attheendoftheexperiment,animalsarekilledandtumor,kidneyandliverarecollected,fixedandparaffinembeddedforhistology[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•bioRxiv.June28,2021.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].RamkumarK,etal.MechanisticevaluationandtranscriptionalsignatureofaglutathioneS-transferaseomega1inhibitor.NatCommun.2016