Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMSU-42011Cat.No.:HY-153832CASNo.:2456434-36-7分?式:C??H??N?O?分?量:382.54作?靶點(diǎn):RAR/RXR;PERK;NOSynthase作?通路:MetabolicEnzyme/Protease;VitaminDRelated/NuclearReceptor;CellCycle/DNADamage;Immunology/Inflammation儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性MSU-42011?種具有?服活性的類視醇X受體(RXR)激動劑。MSU-42011可以有效抑制iNOS以及p-ERK蛋??平的表達(dá)。MSU-42011具有免疫調(diào)節(jié)和抗腫瘤活性。MSU-42011可?于癌癥的研究。體外研究MSU-42011(0-1μM)inhibitsiNOSwithanIC50of158nMinRAW264.7macrophage-likecells[1].MSU-42011(300nM;8h)showsalowinductioneffectonSREBPinHepG2cells[1].MSU-42011(0-5000nM;24h)canactivateRXRαinHepG2cells[1].RT-PCR[1]CellLine:HepG2livercancercellsConcentration:300nMIncubationTime:8hResult:SREBPexpressionrangedfromnochangetoa1.49-foldinductioncomparedtothevehiclecontrol體內(nèi)研究MSU-42011(25mg/kg,PO,for12weeks)significantlyreducesthenumber,sizeandoveralltumorburdenoftumorsinanA/Jmouselungcancermodel.Fewercellsactivelyproliferatedandshowedasignificant[1]reductioninp-ERKcomparedtocontrols.MSU-42011(25mg/kg;PO;1weeklater,intraperitonealinjectionofCarboplatin(HY-17393)(50mg/kg)andpaclitaxel(HY-B0015)(15mg/kg)everyotherweek6times;treatmentfor12weeks)ismosteffectivein1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEreducingtumornumber,tumorsize,andoveralltumorburdenwhencombinedwithC/PintheA/Jmouselungcancermodel.DecreasedmacrophagesinthelungandincreasesCD8+Tcellactivationmarkers[1].MSU42011(100mg/kg;PO;2weekslater,intraperitonealinjection50mg/mouseofanti-PD1andanti-PDL1antibodies,twiceaweek,atotalof22times)reducestumorburdeninamouselungtumormodel[2].AnimalModel:A/Jmice(Intraperitonealinjectedwiththecarcinogenethylcarbamate(0.32mg/injection)for8weeks)[1]Dosage:25mg/kgAdministration:Oraladministration;Oneweekafter,i.p.everyotherweekforatotalof6injectionswithCarboplatin(HY-17393)(50mg/kg)andpaclitaxel(15mg/kg);for12weeksResult:ThenumberandsizeofdetectedlungsurfacetumorsincreasednotinthetreatmentgroupCombineswithC/Pwasmosteffectiveinreducingtumornumber(67%vs.control),tumorsize(76%vs.control),andoveralltumorburden(92%vs.control).AnimalModel:A/Jlungcancermodel(Intraperitonealinjectedwiththecarcinogenethylcarbamate(0.32mg/injection)for8weeks)[2]Dosage:100mg/kgAdministration:Oraladministration;After2weeks,eachmousewasintraperitoneallyinjectedwithanti-PD1andanti-PDL1antibodiesatarateof50μg/mouse,twiceaweekforatotalof22timesResult:Showedthatanincreaseintheratioofanti-tumorCD8TcellstoCD4,CD25TcellsresultedinasignificantreductionintumorvolumecomparedtoMSU42011oranti-PD(L)1antibodyalone.REFERENCES[1].LealAS,etal.TheRXRAgonistMSU42011IsEffectivefortheTreatmentofPreclinicalHER2+BreastCancerandKras-DrivenLungCancer.Cancers(Basel).2021Oct6;13(19):5004.[2].MoerlandJA,etal.ThenovelrexinoidMSU-42011iseffectiveforthetreatmentofpreclinicalKras-drivenlungcancer.SciRep.2020Dec17;10(1):22244.McePdfHeightCaution:Producthasnotbeenfu