SRT 1460

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Chemical Structure| 925432-73-1 同义名 : -
CAS号 : 925432-73-1
货号 : A548750
分子式 : C26H29N5O4S
纯度 : 95+%
分子量 : 507.6
MDL号 : MFCD19053214
存储条件:

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Sirtuin-1 (SIRT1), a NAD+-dependent deacetylase, is a principal modulator of pathways downstream of calorie restriction that produce beneficial effects on glucose homeostasis and insulin sensitivity. SRT1460 is a potent SIRT1 activator with an EC1.5 (concentration required to increase enzyme activity by 50%) value of 2.9 μM, shows good selectivity for activation of SIRT1 versus SIRT2 and SIRT3 (EC1.5>300 μM), and is more potent than Resveratrol and the closest sirtuin homologues[1]. Treatment with different concentrations of SRT1460 inhibited cell viability in a dose-dependent manner, with all pancreatic cancer cells being more sensitive than the control HPDE cell. SRT1460 was also shown to inhibited cell growth by the Trypan blue exclusion and in the anchorage-independent cell growth assays in Patu8988t[2].
作用机制 SRT1460 binds to the SIRT1 enzyme-peptide substrate complex at an allosteric site amino-terminal to the catalytic domain[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.97mL

0.39mL

0.20mL

9.85mL

1.97mL

0.99mL

19.70mL

3.94mL

1.97mL

参考文献

[1]Milne JC, Lambert PD, Schenk S, et al. Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes. Nature. 2007;450(7170):712-716

[2]Chini CC, Espindola-Netto JM, Mondal G, et al. SIRT1-Activating Compounds (STAC) Negatively Regulate Pancreatic Cancer Cell Growth and Viability Through a SIRT1 Lysosomal-Dependent Pathway. Clin Cancer Res. 2016;22(10):2496-2507