Tenovin-1

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Chemical Structure| 380315-80-0 同义名 : -
CAS号 : 380315-80-0
货号 : A152615
分子式 : C20H23N3O2S
纯度 : 98%
分子量 : 369.48
MDL号 : MFCD02914760
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
溶解度 :

DMSO: 105 mg/mL(284.18 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
生物活性
描述 Tenovin-1, functioning as a p53 activator, shields p53 from degradation facilitated by MDM2. Its mechanism involves the inhibition of protein deacetylating activities of SirT1 and SirT2. Additionally, Tenovin-1 serves as an inhibitor of dihydroorotate dehydrogenase (DHODH)[1][2].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
MCF7 cells 10 μM Function assay 6 h Inhibition of SirT1 assessed as increase in p53 expression in human MCF7 cells at 10 uM after 6 hrs by Western blotting 22304848
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.71mL

0.54mL

0.27mL

13.53mL

2.71mL

1.35mL

27.07mL

5.41mL

2.71mL
参考文献

[1]Lain S, et al. Discovery, in vivo activity, and mechanism of action of a small-molecule p53 activator. Cancer Cell. 2008;13(5):454-463.

[2]Ladds MJGW, et al. Exploitation of DHODH and p53 activation as therapeutic targets - a case study in polypharmacology [published online ahead of print, 2020 Sep 8]. J Biol Chem. 2020;jbc.RA119.012056.

[3]Marx C, et al. The sirtuin 1/2 inhibitor tenovin-1 induces a nonlinear apoptosis-inducing factor-dependent cell death in a p53 null Ewing's sarcoma cell line. Invest New Drugs. 2017 Nov 18.

[4]Yoon KB, et al. Induction of Nuclear Enlargement and Senescence by Sirtuin Inhibitors in Glioblastoma Cells. Immune Netw. 2016 Jun;16(3):183-8.

[5]Grbesa I, et al. Expression of sirtuin 1 and 2 is associated with poor prognosis in non-small cell lung cancer patients. PLoS One. 2015 Apr 27;10(4):e0124670.