Salermide
CAS号 | 1105698-15-4 | 货号 | BCP19469 |
中文名 | Salermide | ||
英文名 | Salermide | ||
中文别名 | |||
英文别名 | |||
分子式 | C26H22N2O2 | 分子量 | 394.47 |
生物活性 | InVitro: Salermide shows a dose-dependent inhibition that rises to 80% at 90 μM and 25 μM against Sirt1 and Sirt2, respectively. Salermide can prompt tumour-specific cell death in a wide range of human cancer cell lines derived from leukaemia (MOLT4, KG1A, K562), lymphoma (Raji), colon (SW480) and breast (MDA-MB-231). Incubation with 100 μM Salermide alone results in an increase of cytosolicactivated caspase 3 and a decrease of mitochondrialcytochrome. Salermide alone can induce apoptosis through both extrinsic and intrinsic pathways. Salermide had several antitumorigenic advantages over the earlier described class III HDAC inhibitors: firstly, it mimics the universal proapoptotic effect on cancer samples exhibited by the classical class I, II and IV HDAC inhibitors, and secondly, its proapoptotic effect is cancer-specific. InVivo: Salermide is well tolerated by mice at concentrations up to 100 μM. Salermide's mechanism of action in vivo is specifically mediated by Sirt1. Intraperitone | ||
信号通路 | Cell Cycle/DNA Damage Epigenetics | ||
靶 点 | Sirtuin |
结构式
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