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Tenovin-3

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Chemical Structure| 1011301-27-1 同义名 : -
CAS号 : 1011301-27-1
货号 : A501104
分子式 : C18H21N3OS
纯度 : 99%+
分子量 : 327.444
MDL号 : MFCD25976437
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(91.62 mM)，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
靶点

  • SIRT2
描述 Tenovin-3 is a potent p53 activator. It increase p53 levels, followed increased p21 expression, in MCF-7 cells treated for 6 hr at 10μM, increased K40 Ac-tubulin levels in H1299 cells treated for 16 hr at 10μM and inhibited the deacetylase activities of purified sirt2[4]. The activation of Tenovin-3 on p53 may due to its inhibitory effect on sirtuin[5]. Tenovin-3 exhibited anti-virus activity on vaccinia virus (VV) and La Crosse virus (LACV) with EC50 values of 2.72μM and 2.19μM, respectively[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.05mL

0.61mL

0.31mL

15.27mL

3.05mL

1.53mL

30.54mL

6.11mL

3.05mL
参考文献

[1]Lain S, Hollick JJ, et al. Discovery, in vivo activity, and mechanism of action of a small-molecule p53 activator. Cancer Cell. 2008 May;13(5):454-63.

[2]McCarthy AR, Pirrie L, et al. Synthesis and biological characterisation of sirtuin inhibitors based on the tenovins. Bioorg Med Chem. 2012 Mar 1;20(5):1779-93.

[3]Burgeson JR, Moore AL, et al. SAR analysis of a series of acylthiourea derivatives possessing broad-spectrum antiviral activity. Bioorg Med Chem Lett. 2012 Jul 1;22(13):4263-72.

[4]Lain S, Hollick JJ, Campbell J, Staples OD, Higgins M, Aoubala M, McCarthy A, Appleyard V, Murray KE, Baker L, Thompson A, Mathers J, Holland SJ, Stark MJ, Pass G, Woods J, Lane DP, Westwood NJ. Discovery, in vivo activity, and mechanism of action of a small-molecule p53 activator. Cancer Cell. 2008 May;13(5):454-63. doi: 10.1016/j.ccr.2008.03.004. PMID: 18455128; PMCID: PMC2742717.

[5]McCarthy AR, Pirrie L, Hollick JJ, Ronseaux S, Campbell J, Higgins M, Staples OD, Tran F, Slawin AM, Lain S, Westwood NJ. Synthesis and biological characterisation of sirtuin inhibitors based on the tenovins. Bioorg Med Chem. 2012 Mar 1;20(5):1779-93. doi: 10.1016/j.bmc.2012.01.001. Epub 2012 Jan 12. PMID: 22304848.

[6]Burgeson JR, Moore AL, Boutilier JK, Cerruti NR, Gharaibeh DN, Lovejoy CE, Amberg SM, Hruby DE, Tyavanagimatt SR, Allen RD 3rd, Dai D. SAR analysis of a series of acylthiourea derivatives possessing broad-spectrum antiviral activity. Bioorg Med Chem Lett. 2012 Jul 1;22(13):4263-72. doi: 10.1016/j.bmcl.2012.05.035. Epub 2012 May 17. PMID: 22664128.