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Tenovin-1

CAS No. : 380315-80-0

MCE 国际站：Tenovin-1

产品活性：Tenovin-1 是 sirtuin 1 和 sirtuin 2 的抑制剂，同时可激活 p53，具有潜在的癌症研究的潜力。

研究领域：Apoptosis  |  Metabolic Enzyme/Protease  |  Cell Cycle/DNA Damage  |  Epigenetics  |  Autophagy

作用靶点：MDM-2/p53  |  Dihydroorotate Dehydrogenase  |  Sirtuin  |  Autophagy

In Vitro: Tenovin-1 protects p53 from mdm2-mediated degradation with little effect on p53 synthesis. Tenovin-1 targets a factor(s) upstream of p53 that not only modulates p53 function but also other cellular pathways. Tenovin-1 (10 μM) inhibits SirT2 deacetylase activity.
Tenovin-1 (1-10 μM) induces a bell-shaped concentration-dependent cell death in SK-N-MC cells. Tenovin-1 alters the gene and protein expression of Bcl-2 family members. However, Tenovin-1 has a more powerful effect both on mRNA and protein expression levels at a lower concentration than does the higher concentration. Furthermore, Tenovin-1-induced cytotoxic effects depend on caspases in p53 wild-type WE-68 cells, but not in p53 null SK-N-MC cells. AIF plays a major role in tenovin-1-induced cell death in p53 null SK-N-MC cells, but not in p53 wild-type WE-68 cells. Reactive oxygen species are also involved in tenovin-1-mediated cell death in SK-N-MC cells. In addition, Tenovin-1 causes DNA damage in SK-N-MC cells. Tenovin-1 (5 μM) increases the nuclear size in glioblastoma cells and rat primary astrocytes. Tenovin-1 induces cellular senescence, wich does not appear to be related to cell death.
Tenovin-1 (10 μM) reduces proliferation and anchorage independent growth of NSCLC cells. Tenovin-1 also inhibits cell growth of H358 lung cancer cells.

In Vivo: Tenovin-1 (92 mg/kg, i.p.) reduces growth of tumors in SCID mice derived from BL2 cells or ARN8 cells.

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