中文名 | Inauhzin |
英文名 | Inauhzin |
别名 | 化合物INAUHZIN SIRT1抑制剂(INAUHZIN) |
英文别名 | INAUHZIN Inauhzin Inauhzin(INZ) 10-[1-Oxo-2-(2H-1,2,4-triazino[5,6-b]indol-3-ylthio)butyl]-10H-phenothiazine 2-(9H-[1,2,4]TRIAZINO[6,5-B]INDOL-3-YLTHIO)-1-(10H-PHENOTHIAZIN-10-YL)BUTAN-1-ONE 2-((5H-[1,2,4]Triazino[5,6-b]indol-3-yl)thio)-1-(10H-phenothiazin-10-yl)butan-1-one 1-Phenothiazin-10-yl-2-(9H-1,3,4,9-tetraaza-fluoren-2-ylsufanyl)-butan-1-one (Inauhzin) 10-[1-Oxo-2-(2H-1,2,4-triazino[5,6-b]indol-3-ylthio)butyl]-10H-phenothiazine Inauhzin(INZ) |
CAS | 309271-94-1 |
化学式 | C25H19N5OS2 |
分子量 | 469.58 |
密度 | 1.50±0.1 g/cm3(Predicted) |
沸点 | 773.6±70.0 °C(Predicted) |
溶解度 | DMSO: 21 mg/mL |
酸度系数 | 10.24±0.50(Predicted) |
存储条件 | -20℃ |
体外研究 | Inauhzin (10 µM) induces p53 levels as effectively as actinomycin D (10 nM), and mediates p53-dependent cytotoxicity through its specific functional groups in human lung carcinoma H460 cells. Inauhzin (2 µM) 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 HCT116 p53+/+ 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 (30 mg/kg, i.p.) effectively induces apoptosis and suppresses tumour growth of H460 xenograft harbouring p53. Inauhzin (30 mg/kg, i.p.) reduces the HCT116 tumor volume by appr 70%. Inauhzin (15 mg/kg) in combination with 150 mg/kg of Nutlin-3 demonstrates a significant synergy on p53 induction, apoptosis and tumor suppression of HCT116 p53+/+ xenografts. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.13 ml | 10.648 ml | 21.296 ml |
5 mM | 0.426 ml | 2.13 ml | 4.259 ml |
10 mM | 0.213 ml | 1.065 ml | 2.13 ml |
5 mM | 0.043 ml | 0.213 ml | 0.426 ml |
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