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Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEApoptin-derivedpeptideCat.No.:HY-P10090CASNo.:2232156-31-7分子式:C???H???N??O??S分子量:5177.33Sequence:Met-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Lys-Pro-Pro-Ser-Lys-Lys-Arg-Ile-Arg-Ile-Gly-Ile-Ala-Gly-Ile-Thr-Ile-Thr-Leu-Ser-Leu-Arg-Pro-Arg-Thr-Ala-Lys-Arg-Arg-Ile-Arg-LeuSequenceShortening:MGRKKRRQRRRKPPSKKRIRIGIAGITITLSLRPRTAKRRIRL作用靶點(diǎn): Akt;PI3K;Apoptosis作用通路: PI3K/Akt/mTOR;Apoptosis儲(chǔ)存方式: PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Apoptin-derivedpeptide是一種抗癌活性多肽,具有細(xì)胞毒性。Apoptin-derivedpeptide通過調(diào)節(jié)PI3K/AKT/ARNT信號(hào)而促進(jìn)胃癌細(xì)胞的凋亡(apoptosis)和壞死(necrosis)。在細(xì)胞內(nèi),Apoptin-derivedpeptide抑制癌細(xì)胞侵襲和遷移,并抑制PI3K的亞基p85的表達(dá)和磷酸化,進(jìn)一步抑制胃癌發(fā)展有關(guān)的PI3K/AKT通路[1]。體外研究Apoptin-derivedpeptide(40-100μg/mL,24h)promotesARNTdown-regulationbyinhibitingthePI3K/AKTsignalingpathwaytoreverseCDDPresistanceinSGC-7901/CDDPcells[1].Apoptin-derivedpeptide(10-30μg/mL,24h)inhibitsthemigrationandinvasioninSGC-7901,SGC-7901/CDDPandMGC-803cells[1].Apoptin-derivedpeptide(30-60μg/mL,24h)increasestheCDDPsensitivityofSGC-7901/CDDPcells[1].Apoptin-derivedpeptide(10-20μg/mL,24h)increasestheG2/MphasepopulationandinducesapoptosisinSGC-7901andSGC-7901/CDDPcells.[1].Apoptin-derivedpeptide(10-70μg/mL,4-24h)hasanexcellentinhibitoryeffectinSGC-7901andSGC-7901/CDDPcells.CellViabilityAssay[1]CellLine:HEK293,SGC-7901,SGC-7901/CDDP1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEConcentration:10μg/mL,20μg/mL,30μg/mL,40μg/mL,50μg/mL,60μg/mL,70μg/mLIncubationTime:4h,6h,8h,12h,18h,24hResult:ProducedlargeeffectsinbothSGC-7901andSGC-7901/CDDPcellsat60μg/mLfor6handhadnoobviouseffectonHEK293cells.ApoptosisAnalysis[1]CellLine:SGC-7901,SGC-7901/CDDPConcentration:30μg/mL,60μg/mLIncubationTime:24hResult:InducedSGC-7901cellapoptosisinaconcentrationdependentmanner.InducedconsiderableapoptoticcelldeathinSGC-7901/CDDPcellsinastrongtime-anddose-dependentfashion.CellCycleAnalysis[1]CellLine:SGC-7901,SGC-7901/CDDPConcentration:10μg/mL,20μg/mLIncubationTime:24hResult:IncreasetheG2/Mphasepopulation.CellInvasionAssay[1]CellLine:SGC-7901,SGC-7901/CDDP,MGC-803Concentration:10μg/mL,20μg/mL,30μg/mLIncubationTime:48hResult:Significantlyreducedthenumberofinvasivecells.CellMigrationAssay[1]CellLine:SGC-7901,SGC-7901/CDDP,MGC-803Concentration:10μg/mL,20μg/mL,30μg/mLIncubationTime:48hResult:EffectivelyinhibitedthemigrationabilityofMGC-803,SGC-7901,andSGC-7901/CDDPcellsinadose-dependentmanner.2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEWesternBlotAnalysis[1]CellLine:SGC-7901,SGC-7901/CDDPConcentration:40μg/mL,60μg/mL,80μg/mL,100μg/mLIncubationTime:24hResult:Significantlydown-regulatedthephosphorylationofp85(p-p85)andAKT(p-AKT)proteinsatconcentrationsfrom40μg/mLto100μg/mL.Down-regulatedtheexpressionofMDR1andARTNinApoptin-derivedpeptide-treatedSGC-7901/CDDPcells.Notablydecreasedp85andAKTactivities.REFERENCESZhouD,etal.Apoptin-derivedpeptidereversescisplatinresistanceingastriccancerthroughthePI3K-AKTsignalingpathway[J].CancerMedicine,2018,7(4):1369-1383.McePdfHeightCaution:Producthasnotbeen

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