Inauhzin Inauhzin;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);10-[1-Oxo-2- 309271-94-1
Inauhzin(INZ) is a novel small molecule that effectively reactivates p53 by inhibiting SIRT1 activity, promotes p53-dependent apoptosis of human cancer cells without causing apparently genotoxic stress(IC50=3 uM, in A549 cell).
IC50 value: 3 uM(A549 cell); 5.4 uM (H460 cell) [1]
Target: SIRT1
in vitro: Inauhzin effectively reactivates p53 by inhibiting SIRT1 activity, promotes p53-dependent apoptosis of human cancer cells without causing apparently genotoxic stress. Moreover, INZ stabilizes p53 by increasing p53 acetylation and preventing MDM2-mediated ubiquitylation of p53 in cells, though not directly in vitro. Remarkably, INZ inhibits cell proliferation, induces senescence and tumour-specific apoptosis [1].
in vivo: represses the growth of xenograft tumours derived from p53-harbouring H460 and HCT116 cells without causing apparent toxicity to normal tissues and the tumour-bearing SCID mice [1].
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