UBCS039
产品说明书
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同义名 : | - |
| CAS号 : | 358721-70-7 | |
| 货号 : | A1177029 | |
| 分子式 : | C16H13N3 | |
| 纯度 : | 99%+ | |
| 分子量 : | 247.29 | |
| MDL号 : | MFCD00206184 | |
| 存储条件： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 描述 | Sirtuin 6 (SIRT6) is a member of the NAD+-dependent class III deacetylase sirtuin family, which plays a key role in cancer by controlling transcription, genome stability, telomere integrity, DNA repair, and autophagy[1]. UBCS039 is the first synthetic SIRT6 activator with EC50 of 38 μM, which can induce time-dependent activation of autophagy in various human tumor cell lines[2]. UBCS039 (75 μM) induced a time-dependent deacetylation of histone H3K9 in H1299 non-small cell lung cancer. UBCS039 also triggered deacetylation of histone H3K56 in HT1080 cells. Moreover, knockdown of SIRT6, by increasing in a time dependent manner H3K9 acetylation levels, exerted opposite effects compared to UBCS039 treatment. Collectively, these results demonstrated that UBCS039 is a specific activator of SIRT6 in several human tumor models. UBCS039 (75 μM) enhanced, in a time-dependent manner, LC3B conversion from LC3B form I (18 kDa) to an autophagosome-associating form, LC3 form II (16 kDa) in both human H1299 and HeLa cell lines. UBCS039-induced autophagosome accumulation was also observed in HT1080 fibrosarcoma cells stably transfected with EGFP-LC3B fusion protein, thus indicating ageneral effect on autophagy upon activation of SIRT6. Notably, UBCS039 treatment increased AMP-activated protein kinase (AMPK) phosphorylation in H1299 cells, indicating UBCS039 induced autophagy via AMPK signaling pathway activation[1]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
4.04mL 0.81mL 0.40mL |
20.22mL 4.04mL 2.02mL |
40.44mL 8.09mL 4.04mL |
| 参考文献 |
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