JAK1-2-IN-3-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEJAK1/2-IN-3Cat.No.:HY-180274分⼦式:C₂₂H₁₃Cl₂N₅O₅分⼦量:498.28作⽤靶点:JAK;Apoptosis;Caspase;Bcl-2Family作⽤通路:Epigenetics;JAK/STATSignaling;ProteinTyrosineKinase/RTK;StemCell/Wnt;Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性JAK1/2-IN-3⼀种JAK1和JAK2抑制剂，其IC50值分别为14.73nM和10.03nM。JAK1/2-IN-3可诱导G2/M期细胞周期阻滞，并通过增加Bax和caspase3/7⽔平以及降低Bcl2表达来诱导内性凋亡(apoptosis)。JAK1/2-IN-3可⽤于⽩⾎病、乳腺癌和结肠癌的研究。IC50&TargetJAK1JAK2Caspase3Caspase-714.73nM(IC50)10.03nM(IC50)BaxBcl-2体外研究JAK1/2-IN-3(Compound3i)inhibitsHT-29,MCF-7,HL-60andHCT-116cells,withIC50valuesof1.02μM,1.87μM,7.92μMand1.27μM,respectively.JAK1/2-IN-3exhibitslowertoxicitytowardnormalWI-38cells(IC50:19.93μM)[1].JAK1/2-IN-3(1.02µM;24hours)inducesapoptosisinHT-29cells[1].JAK1/2-IN-3(1.02µM;24hours)causesinductionofG2/McellcyclearrestinHT-29cells[1].JAK1/2-IN-3(1.02µM;48hours)increasesBaxandcaspase3/7levelsandreducesBcl2expressioninHT-29cells[1].ApoptosisAnalysis[1]CellLine:HT-29Concentration:1.02µMIncubationTime:24hours1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:Significantlyincreasedapoptosiswitha24.39%totalapoptosisrateanda16.9%lateapoptoticrate.CellCycleAnalysis[1]CellLine:HT-29Concentration:1.02µMIncubationTime:24hoursResult:Ledtoa5.55-foldincreaseintheG2/MpopulationcomparedtotheuntreatedHT-29cells,accompaniedbyanotabledropintheG0/G1andSphasepopulationsbyaround24.4%and38.6%,respectively.RT-PCR[1]CellLine:HT-29Concentration:1.02µMIncubationTime:48hoursResult:Showeda3.34-foldupregulationofBax,a0.26-folddownregulationofBcl2,and5.96-foldand9.00-foldincreasesincaspase-3andcaspase-7,respectively.REFERENCES[1].FaggalSI,etal.Design,synthesis,andanticancerevaluationofnewPhenylpyrazolonederivatives:DualJAK1/JAK2inhibition,apoptosis-inducingactivity,andmolecularmodellingstudies.BioorgChem.2025;167:109268.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseon