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UBCS039

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Chemical Structure| 358721-70-7 同义名 : -
CAS号 : 358721-70-7
货号 : A1177029
分子式 : C16H13N3
纯度 : 99%+
分子量 : 247.294
MDL号 : MFCD00206184
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(424.59 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
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
1mg 5mg 10mg

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

[1]Iachettini S, Trisciuoglio D, Rotili D, et al. Pharmacological activation of SIRT6 triggers lethal autophagy in human cancer cells. Cell Death Dis. 2018;9(10):996

[2]You W, Rotili D, Li TM, et al. Structural Basis of Sirtuin 6 Activation by Synthetic Small Molecules. Angew Chem Int Ed Engl. 2017;56(4):1007-1011