ML162-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEML162Cat.No.:HY-100002CASNo.:1035072-16-2分?式:C??H??Cl?N?O?S分?量:477.4作?靶點:GlutathionePeroxidase;Ferroptosis作?通路:MetabolicEnzyme/Protease;Apoptosis儲存?式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(209.47mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.0947mL10.4734mL20.9468mL5mM0.4189mL2.0947mL4.1894mL10mM0.2095mL1.0473mL2.0947mL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(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：(為保證實驗結(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)實驗的?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%cornoilSolubility:≥2.5mg/mL(5.24mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性ML162?種共價?胱?肽過氧化物酶4(GPX4)抑制劑。ML162對表達突變RAS癌因的細胞系具有選擇性的致死作?。體外研究ML162(compound1a)showsnanomolarpotenciesagainsttwoHRASG12Vexpressingcelllines,withIC50valuesof25nMand578nMforHRASG12V-expressingandwild-typeBJfibroblasts,respectively[1].ML162(8μM;24hours)treatmentincreasestheexpressionofp62andNrf2inchemoresistantHN3RandHN3-rslRcells,inactivatesKeap1,andincreasesexpressionofthephospho-PERK-ATF4-SESN2pathway[2].ML162inducestheheadandneckcancer(HNC)celldeathtovaryingdegrees,withparentalHN3cellsmoresensitiveandcisplatin-resistant(HN3R)andacquiredRSL3-resistant(HN3-rslR)cellslesssensitive[2].WesternBlotAnalysis[2]CellLine:HN3RcellsConcentration:8μMIncubationTime:24hoursResult:Increasedtheexpressionofp62andNrf2inchemoresistantHN3RandHN3-rslRcells.REFERENCES[1].MichelWe?wer,etal.Developmentofsmall-moleculeprobesthatselectivelykillcellsinducedtoexpressmutantRAS.BioorgMedChemLett.2012Feb15;22(4):1822-6.[2].DaihaShin,etal.Nrf2inhibitionreversesresistancetoGPX4inhibitor-inducedferroptosisinheadandneckcancer.FreeRadicBiolMed.2018Dec;129:454-462.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuse