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Inauhzin  ≥98%(HPLC)

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包装规格：1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO(20mg/mL 加热 超声)
产品描述：基本信息 产品编号：I10168 产品名称：Inauhzin CAS: 309271-94-1   储存条件 粉末 -20℃ 四年     分子式： C25H19N5Os2 溶于液体 -80℃ 两年 分子量 469.58 -20℃ 一个月 化学名：  2-((5H-[1,2,4]triazino[5,6-b]indol-3-yl)thio)-1-(10H-phenothiazin-10-yl)butan-1-one   Solubility (25°C)   体外 DMSO 94mg/mL (200.17mM) Ethanol Insoluble Water Insoluble 体内 现配现用   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.1296mL 10.6478mL 21.2956mL 5mM 0.4259mL 2.1296mL 4.2591mL 10mM 0.2130mL 1.0648mL 2.1296mL 50mM 0.0426mL 0.2130mL 0.4259mL   生物活性 产品描述 一种SirT1/IMPDH2的双重抑制剂，同时为p53的激活剂。 靶点/IC50 SIRT1 () p53 ()   体外研究 Inauhzin (10µM) induces p53 levels as effectively as actinomycin D (10nM), and mediates p53-dependent cytotoxicity through its specific functional groups in human lung carcinoma H460 cells. Inauhzin (2µM) induces p53 level and activity as well as p53-dependent apoptosis. Inauhzin also stabilizes p53 and inhibits its ubiquitylation. Inauhzin induces acetylation of p53 in H460 cells, but not tubulin, which is affected by knockdown of SIRT1. Inauhzin (0-2 µM) significantly enhances the expression level and activity of p53 in HCT116p53+/+ cells and enhances the expression level and activity of p53 in H460 cells in a dose-dependent manner. Inauhzin and Nutlin-3 demonstrate synergistic cytotoxicity in the Nutlin-3 low-sensitive cells. Inauhzin and Nutlin-3 synergistically induce p53-dependent apoptosis. Inauhzin targets both SirT1 and IMP dehydrogenase 2 (IMPDH2), and acts as a potent p53 activator.   体内研究 Inauhzin (30mg/kg, i.p.) effectively induces apoptosis and suppresses tumour growth of H460 xenograft harbouring p53. Inauhzin (30mg/kg, i.p.) reduces the HCT116 tumor volume by appr 70%. Inauhzin (15mg/kg) in combination with 150mg/kg of Nutlin-3 demonstrates a significant synergy on p53 induction, apoptosis and tumor suppression of HCT116p53+/+ xenografts.   推荐实验方法(仅供参考) 细胞实验： Cell Assay The cell counting kit is used to assess cell growth. Cell suspensions are seeded at 5000 cells per well in 96-well culture plates and incubated overnight at 37°C. Compounds are added into the plates and incubated at 37°C for 72 h. Cell growth inhibition is determined by adding WST-8 at a final concentration of 10% to each well, and the absorbance of the samples is measured at 450nm using a Microplate Reader.   动物实验:   Animal Administration Five-weeks-old female SCID mice are housed in a BSL2 environment. Mice are subcutaneously inoculated with 5×106 H460 or 3×106 HCT116 cells. Tumour growth is monitored every other day with electronic digital calipers in two dimensions.Tumour volume is calculated with the formula: tumour volume (mm3) = (length × width2)/2. When the mean tumour volume reaches approximately 100 mm3 after 7-9 days, animals are dosed by i.p. injection with vehicle (5% DMSO) or Inauhzin. Inhibition of tumour growth is calculated on the last day of treatment. To detect p53 activation in vivo, tumours are harvested and disrupted in RIPA buffer containing a protease inhibitor mixture. Tumour lysates are analysed by IB. Cell proliferation in tumours is assessed by BrdU labeling followed by Immunostaining. 200mg/kg body weight of BrdU is administrated to mice via i.p. injection 2 h before mice are sacrificed. Apoptosis is examined by TUNEL staining, using the Fluorescein In situ cell death detection kit
保存条件：-20℃

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