Cambinol,14513-15-6

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Cambinol

CAS No. : 14513-15-6

MCE 国际站：Cambinol

产品活性：Cambinol 是一种 SIRT1 和 SIRT2 的抑制剂，IC₅₀ 值分别为 56 μM 和 59 μM。Cambinol 是中性鞘磷脂酶 (N-SMase) 的抑制剂(外泌体抑制剂)。

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

作用靶点：Sirtuin  |  Apoptosis  |  Phospholipase

In Vitro: Cambinol inhibits NAD-dependent deacetylase activity of human SIRT1 and SIRT2. Inhibition of SIRT1 activity with cambinol during genotoxic stress leads to hyperacetylation of key stress response proteins and promotes cell cycle arrest. Treatment of BCL6-expressing Burkitt lymphoma cells with cambinol as a single agent induces apoptosis, which is accompanied by hyperacetylation of BCL6 and p53. Cambinol has only weak inhibitory activity against SIRT5 (42% inhibition at 300 μM) and no activity against SIRT3.

In Vivo: Cambinol is well tolerated in mice (100 mg/kg) and inhibits growth of Burkitt lymphoma xenografts. No significant weight loss occurs in cambinol-treated animals relative to controls. Inhibitors of NAD-dependent deacetylases may constitute novel anticancer agents.

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