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)
相关类别:
细胞生物学试剂;小分子抑制剂，天然产物;小分子抑制剂;Inhibitors
沸点
773.6±70.0 °C(Predicted)
密度
1.50±0.1 g/cm3(Predicted)
酸度系数(pKa)
10.24±0.50(Predicted)
生物活性
Inauhzin是具有细胞透性的SIRT1抑制剂，IC50为0.7-2 μM，可通过抑制SIRT1脱乙酰活性重新激活p53。
靶点
Target Value
SIRT1
()
p53
()
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.
