DU-14-PTP1B-TC-PTP-PROTAC-生命科學(xué)試劑-MCE-8913

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEDU-14(PTP1B/TC-PTPPROTAC)Cat.No.:HY-164864CASNo.:3053413-58-1分?式:C??H??BrF?N?O??PS分?量:1505.46作?靶點(diǎn):PROTACs;STAT作?通路:PROTAC;JAK/STATSignaling;StemCell/Wnt儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性DU-14(PTP1B/TC-PTPPROTAC)?種有效的和選擇性的PTP1B和TC-PTP雙重PROTAC降解劑，對PTP1B和TC-PTP磷酸酶活性的IC50分別為24.2nM和30.1nM。DU-14(PTP1B/TC-PTPPROTAC)可以增強(qiáng)IFN-γ信號傳導(dǎo)、促進(jìn)T細(xì)胞活化，具有抗腫瘤的活性。(粉?:PTP1B/TC-PTP抑制劑(HY-171027);??:連接?(HY-W340290);藍(lán)?:E3連接酶配體(HY-112078))IC50&TargetIC50:24.2nM(PTP1B);30.1nM(TC-PTP)[1]體外研究DU-14(PTP1B/TC-PTPPROTAC)(0-1000nM;16h)causesPTP1B/TC-PTPdegradationandpromotesSTAT1phosphorylationinIFN-γ-treatedMC38cells[1].DU-14(PTP1B/TC-PTPPROTAC)(48h)effectivelydegradesTC-PTPandPTP1BinTcellsandpromotestheactivationofTcells[1].WesternBlotAnalysis[1]CellLine:IFN-γtreatedMC38cellsConcentration:0,5,25,125,250,500and1000nMIncubationTime:16hResult:InhibitedthelevelsofPTP1BandTC-PTPinadose-dependentmanner.IncreasedthelevelofpSTAT1/Y701inadose-dependentmanner.體內(nèi)研究DU-14(PTP1B/TC-PTPPROTAC)(25-50mg/kg;intraperitonealinjection;10days)hasantitumoractivityina1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEmousemodelofcoloncancer[1].AnimalModel:C57BL/6micebearingMC38colorectaltumorsintheflanks[1]Dosage:25and50mg/kgAdministration:Intraperitonealinjection(i.p.);10daysResult:EffectivelyrepressedMC38tumorgrowthatdoseof25mg/kg,andresultedinstatictumorgrowthatdoseof50mg/kg.Didnotproducesignificanttoxicity.DegradednearlycompletePTP1BandTC-PTPinwholetumorhomogenates.IncreasedCD8+TcellinfiltratesinMC38tumors.REFERENCES[1].DongJ,etal.SmallMoleculeDegradersofProteinTyrosinePhosphatase1BandT-CellProteinTyrosinePhosphataseforCancerImmunotherapy.AngewChemIntEdEngl.2023May22;62(22):e202303818.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Te