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5-羰基-8-羟基喹啉 |
| CAS No.: |
5852-78-8 |
| 分子式： |
C10H7NO3 |
| 分子量： |
189.17048 |
| 备注： |
中文名称5-羰基-8-羟基喹啉中文同义词8-羟基喹啉-5-羧酸;5-羰基-8-羟基喹啉英文名称5-Carboxy-8-hydroxyquinoline英文同义词5-Carboxy-8-hydroxyquinoline;8-Hydroxyquinoline-5-carboxylicAcid;IOX1;8-hydroxy-5-Quinolinecarboxylicacid;IOX1,>=98%;JMJD2Inhibitor,5-carboxy-8HQ;8-Hydroxyquinoline-5-carboxylicacid95%;JMJD2Inhibitor,5-carboxy-8HQ-CAS5852-78-8-CalbiochemCAS号5852-78-8分子式C10H7NO3分子量189.17EINECS号相关类别小分子抑制剂，天然产物;染料中间体;小分子;Inhibitors;Aromatics,Heterocycles,Pharmaceuticals,Intermediates&FineChemicals;123456Mol文件5852-78-8.mol结构式5-羰基-8-羟基喹啉性质熔点301°C(decomp)沸点464.5±30.0°C(Predicted)密度1.480±0.06g/cm3(Predicted)储存条件2-8°C溶解度DMSO：可溶10mg/mL，澄清酸度系数(pKa)1.82±0.10(Predicted)形态粉末颜色白色至棕色稳定性自购买之日起1年内保持稳定。DMSO中的溶液可在-20°下保存长达3个月。InChIKeyJGRPKOGHYBAVMW-UHFFFAOYSA-N5-羰基-8-羟基喹啉用途与合成方法生物活性IOX1，是2OG氧合酶(2OGoxygenases)的有效广谱抑制剂，包括JmjC去甲基酶。IOX1抑制KDM4C，KDM4E，KDM2A，KDM3A和KDM6B的IC50值分别为0.6μM，2.3μM，1.8μM，0.1μM和1.4μM。IOX1抑制ALKBH5。体外研究IOX1(0-200µM;2hours)inhibitstheproliferationandmigrationofvascularsmoothmusclecells(VSMCs)stimulatedwithangiotensinII(AngII)inaconcentration-dependentmanner.IOX1(200µM;24hours)blocksthecellcycleprogressionofangiotensinII(AngII)-VSMCsbyincreasingthepercentageofcellsintheG0/G1phase.IOX1(50-200µM;2hours)attenuatescyclinD1andupregulatesp21mRNAlevelsinaconcentration-dependent.IOX1(50-200µM;2hours)mediatescyclinD1andp21expressiChemicalbookonbyregainingH3K9me3.CellProliferationAssayCellLine:Vascularsmoothmusclecells(VSMCs)Concentration:50μM,100μM,200μMIncubationTime:Pretreated2hoursResult:Exhibitedadecreaseinproliferationandmigration.CellCycleAnalysisCellLine:Vascularsmoothmusclecells(VSMCs)Concentration:200μMIncubationTime:24hoursResult:SloweddowntheprogressionofthecellcyclefromtheG0/G1totheSphase.RT-PCRCellLine:Vascularsmoothmusclecells(VSMCs)Concentration:50μM,100μM,200μMIncubationTime:2hoursResult:DecreasedcyclinD1mRNAexpressionandincreasedp21mRNAexpression.RT-PCRCellLine:Vascularsmoothmusclecells(VSMCs)Concentration:50μM,100μM,200μMIncubationTime:2hoursResult:EnhancedthetotalproteinlevelsofH3K9me3.体内研究IOX1(5-c-8HQ)(oralgavage;10-20mg/kg;12days)inhibitstumorgrowthandattenuatestheself-renewaloflivercancerstem-likecells(LCSCs)invivo.AnimalModel:Six-week-oldmaleBALB/cnudemiceDosage:10mg/kg,20mg/kgAdministration:12daysResult:Didnotresultinobviousadverseeffectsonmiceasdemonstratedbynobodyweightreductionandnotoxicitytothemajororgansaftertreatment.InhibitedLCSCorthotopicgrafttumorgrowth.SignificantlyreducedtheproteinlevelsofEpCAMandSox9inLCSCorthotopicgrafttumorsnhibitedLCSCorthotopicgrafttumorgrowth.DecreasedKi67-positivetumorcellsandmarkedlyreducedthetumorsphereformationabilitiesofLCSCsinadose-dependentmanner.安全信息 |
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