INAUHZIN
中文名称 | INAUHZIN |
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中文同义词 | SIRT1抑制剂(INAUHZIN);化合物INAUHZIN;INAUHZIN 标准品;2-((5H-[1,2,4]三嗪并[5,6-B]吲哚-3-基)硫基)-1-(10H-吩噻嗪-10-基)丁-1-酮 |
英文名称 | Inauhzin |
英文同义词 | Inauhzin, >=98%;2-((5H-[1,2,4]Triazino[5,6-b]indol-3-yl)thio)-1-(10H-phenothiazin-10-yl)butan-1-one;Inauhzin;1-Phenothiazin-10-yl-2-(9H-1,3,4,9-tetraaza-fluoren-2-ylsufanyl)-butan-1-one (Inauhzin);2-(9H-[1,2,4]TRIAZINO[6,5-B]INDOL-3-YLTHIO)-1-(10H-PHENOTHIAZIN-10-YL)BUTAN-1-ONE;10-[1-Oxo-2-(2H-1,2,4-triazino[5,6-b]indol-3-ylthio)butyl]-10H-phenothiazine;Inauhzin(INZ);10-[1-Oxo-2-(2H-1,2,4-triazino[5,6-b]indol-3-ylthio)butyl]-10H-phenothiazine Inauhzin(INZ) |
CAS号 | 309271-94-1 |
分子式 | C25H19N5OS2 |
分子量 | 469.58 |
EINECS号 | |
相关类别 | 小分子抑制剂,天然产物;小分子抑制剂;细胞生物学试剂;Inhibitors |
Mol文件 | 309271-94-1.mol |
结构式 |
INAUHZIN 性质
沸点 | 773.6±70.0 °C(Predicted) |
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密度 | 1.50±0.1 g/cm3(Predicted) |
储存条件 | Store at -20°C |
溶解度 | DMSO 中≥23.5 mg/mL;不溶于水;不溶于乙醇 |
形态 | 固体 |
酸度系数(pKa) | 10.24±0.50(Predicted) |
颜色 | 浅黄至黄色 |
Target | Value |
SIRT1
() | |
p53
() |
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.
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.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/08/19 | HY-15869 | Inauhzin | 1 mg | 350元 | |
2024/08/19 | HY-15869 | INAUHZIN Inauhzin | 309271-94-1 | 5mg | 650元 |