BRD4-Inhibitor-38-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBRD4Inhibitor-38Cat.No.:HY-170686分?式:C??H??N?O?分?量:338.36作?靶點:InterleukinRelated;TNFReceptor;EpigeneticReaderDomain作?通路:Immunology/Inflammation;Apoptosis;Epigenetics儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性BRD4Inhibitor-38(Compound25)?種具有?服活性的BRD4抑制劑,其對BRD4BD1和BRD4BD2的IC50值分別為3.64μM和0.12μM。BRD4Inhibitor-38具有抗炎活性，其對?氧化氮(NO)?成的IC50值為1.98μM[1]。IC50&TargetBRD4BD1BRD4BD23.64μM(IC50)0.12μM(IC50)體外研究BRD4Inhibitor-38(Compound25)(2.5-20μM;2h)exhibitsanti-inflammatoryactivityinRaw264.7andTHP-1cells[1].RealTimeqPCR[1]CellLine:Raw264.7,THP-1Concentration:2.5,5,10,20μMIncubationTime:2h(stimulatedwithLPS(1μg/mL)andLPS(100ng/mL)+IFN-γ(20ng/mL)for6h.note:Compound25werepre-treatedfor2hbeforestimulatingwithLPSfor6h.)Result:InhibitedthemRNAexpressionofLPS-inducedIL-6andTNF-αinadependentmanner.體內(nèi)研究BRD4Inhibitor-38(Compound25)(25-100mg/kg;p.o.;singledose)exhibitsanti-inflammatoryactivityinamousemodelofacuteinflammationinducedbyLPS(10mg/kg;Singledose)(HY-D1056)[1].AnimalModel:LPS-inducedmousemodelofacuteinflammation[1].1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEDosage:25,50,100mg/kgAdministration:Oraladministration(p.o.)，singledose.AfterLPStreatment(10mg/kg;Singledose)Result:SignificantlyinhibitedtheincreaseofinflammatorygenesIL-6andTNF-αatdosesof50and100mg/kg.Alleviatedlungtissueedema,damage,andlunghemorrhage.Mitigatedkidneydamage,significantlyincreasedtheproportionofnormalrenaltubules,improvedtheinternalbrushborderstructure,reducedrenalinterstitialinflammatorycellinfiltration,anddecreasedthenumberofinterstitialvacuolesatadoseof100mg/kg.REFERENCES[1].ChenS,etal.Marinenaturalproduct-inspireddiscoveryofnovelBRD4inhibitorswithanti-inflammatoryactivity[J].EuropeanJournalofMedicinalChemistry,2024:117193.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly