Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEVCP/p97IN-3Cat.No.:HY-174984分子式:C??H??F?N?O?S分子量:606.69作用靶點(diǎn):p97;Caspase;p62作用通路:CellCycle/DNADamage;Apoptosis;Autophagy儲存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性VCP/p97IN-3是一種VCP/p97變構(gòu)抑制劑。VCP/p97IN-3對VCP顯示出抑制活性，IC50為9nM，對突變型VCP蛋白的IC50分別為12nM(N660K)和19nM(V474A/D649A)。VCP/p97IN-3增加K48泛素化水平和caspase-3的含量。VCP/p97IN-3激活內(nèi)質(zhì)網(wǎng)應(yīng)激和未折疊蛋白反應(yīng)(UPR)。VCP/p97IN-3在RPMI-8226細(xì)胞皮下異種移植小鼠模型中抑制腫瘤生長。VCP/p97IN-3可用于多發(fā)性骨髓瘤的研究[1]。體內(nèi)研究VCP/p97IN-3(Compound38)(50-100mg/kg,i.p.,everyotherday,23days)inhibitstumorgrowthinRPMI-8226cellsubcutaneousxenograftmousemodels[1].AnimalModel:RPMI-8226cellsubcutaneousxenograftmice[1]Dosage:50,100mg/kgAdministration:i.p.everyotherday,23daysResult:IncreasedtheubiquitinofK48andthelevelofcleavedcaspase-3.Activatedendoplasmicreticulum(ER)-stressandtheUPR,asassessedbyincreasesinphosphorylated-eIF2α(p-eIF2α),activationtranscriptionfactor4(ATF4),74andglucose-regulatedprotein(BiP/GRP78).ActivatedtheDNAdamageresponseasobservedfromthe2.5-foldincreaseinphosphorylatedHistone2A(H2A.X).Reducedp62levels.ShowedaTGIof73%onday23.Sufferedamean10%lossinbodyweight.1/2 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEREFERENCES[1].GreenN,etal.AntitumorEfficacyof1,2,4-Triazole-BasedVCP/p97AllostericInhibitors.JMedChem.2025Jul24;68(14):14465-14494.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;021-58955