p-nitro-Cyclic Pifithrin-α

中文名称Pifithrin-α,p-nitro,cyclic中文同义词5,6,7,8-四氢-2-(4-硝基苯基)咪唑并[2,1-b]苯并噻唑;PIFITHRIN-Α,P-NITRO,CYCLIC;化合物PIFITHRIN-Α,P-NITRO,CYCLIC;PIFITHRIN-Α(P53抑制剂)英文名称Pifithrin-α,p-nitro,cyclic英文同义词Pifithrin-α,p-nitro,cyclic;p-nitro-CyclicPifithrin-α;Pifithrin-alpha,p-Nitro,Cyclic;2-(4-Nitro-phenyl)-5,6,7,8-tetrahydro-benzo[d]imidazo[2,1-b]thiazole;p-nitroCyclicPifithrin-.alpha.;Cyclicpifithrin-α-p-nitro;Pifithrin-α,p-Nitro,Cyclic-CAS60477-38-5-Calbiochem;p-Nitro-CyclicPifithrin-aCAS号60477-38-5分子式C15H13N3O2S分子量299.35EINECS号相关类别Mol文件60477-38-5.mol结构式Pifithrin-α,p-nitro,cyclic性质熔点233-234°C(Solv:N,N-dimethylformamide(68-12-2);water(7732-18-5))密度1.53±0.1g/cm3(Predicted)储存条件-20C溶解度二甲基甲酰胺中≤1mg/ml形态黄色固体酸度系数(pKa)6.14±0.20(Predicted)Pifithrin-α,p-nitro,cyclic用途与合成方法生物活性Pifithrin-α,p-Nitro,Cyclic(PFN-α)，是细胞通透性的p53抑制剂。Pifithrin-α,p-Nitro,Cyclic对暴露于Etoposide的皮层神经元的保护作用比Pifithrin-α强一个数量级(ED50=30nM)。Pifithrin-α,p-Nitro,Cyclic也作为p53转录后活性抑制剂。Pifithrin-α,p-Nitro,Cyclic不阻止p53上的S15残基磷酸化。体外研究Pifithrin-α,p-Nitro,Cyclic(PFN-α)efficientlyblocksp53-triggeredcelldeathandp21/WAF1expressionincorticalneuronsexposedtoetoposideatconcentrationsoneordermagnitudelowerthanthatinPFT-α.体内研究Intraocularinjectionofpifithrin-αslightlyincreasessurvivalofretinalganglioncell(RGC)attheconcentrationof6μMbutnotat0.06μM.Pifithrin-α,p-Nitro,Cyclic(PFN-α)isnoteffectiveinvivo,evenat6μM.Pifithrin-α,p-Nitro,Cyclicshowsthehalf-life(t1/2)of6hours(whenincubatedinbiologicalconditions).