GPX4-IN-3-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGPX4-IN-3Cat.No.:HY-141809分?式:C??H??ClN?O?S分?量:530.04作?靶點:GlutathionePeroxidase;Ferroptosis作?通路:MetabolicEnzyme/Protease;Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:67.5mg/mL(127.35mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.8867mL9.4333mL18.8665mL5mM0.3773mL1.8867mL3.7733mL10mM0.1887mL0.9433mL1.8867mL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，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>>90%(20%SBE-β-CDinsaline)Solubility:6.75mg/mL(12.73mM);Suspendedsolution;Needultrasonic2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥6.75mg/mL(12.73mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性GPX4-IN-3(26a)有效的?胱?肽過氧化物酶4(GPX4)抑制劑，可選擇性誘導鐵死亡(ferroptosis)。GPX4-IN-3(26a)在1μM的濃度可抑制GPX471.7%活性。體外研究GPX4-IN-3(26a)exhibitsIC50valuesof0.78μM,6.9μM,0.15μMand4.73μMin4T1,MCF-7,HT1080andHT1080(withFer-1)cells,respectively[1].GPX4-IN-3(26a)exhibitsoutstandingGPX4inhibitoryactivitywithapercentinhibitionupto71.7%at1.0μMcomparedto45.9%ofRSL-3[1].GPX4-IN-3(26a)couldsignificantlyinducelipidperoxide(LPO)increaseandeffectivelyinduceferroptosiswithsatisfactoryselectivity[1].GPX4-IN-3(26a)ismorelikelytoinduceferroptosisthroughtheaccumulationofintracellularperoxidesviainhibitingGPX4activity[1].GPX4-IN-3(26a)significantlyincreasedthelevelofROSin4T1cells,whichcouldalsobereversedbyFerrostatin-1(fer-1)[1].體內(nèi)研究GPX4-IN-3(26a)exertesantitumoractivityandgoodbiologicalsafetyinvivo[1].AnimalModel:Mouse4T1xenograftmodel[1].Dosage:15and30mg/kg.Administration:Intravenousinjection,everytwodaysforatotaloffivetimes.Result:Significantlysuppresstumorgrowthwithatumorgrowthinhibition(TGI)valueof33.2and55.1%at15and30mg/kg,respectively.REFERENCES[1].CongjunXu,etal.DiscoveryofaPotentGlutathionePeroxidase4InhibitorasaSelectiveFerroptosisInducer.JMedChem.2021Sep23;64(18):13312-13326.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.For