SRT 1460 是一种有效的 Sirtuin-1 (SIRT1) 激动剂，其 EC1.5 值为 2.9 μM。与对 SIRT2 和 SIRT3 (EC1.5>300 μM) 相比，SRT 1460 对 SIRT1 有很好的选择性，并且比白藜芦醇和相近 sirtuin 同系物更为有效。
货号:ajcx38752
CAS:925432-73-1
分子式:C26H29N5O4S
分子量：507.6
溶解度:DMSO : 10 mg/mL (19.70 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

SRT 1460, a potent Sirtuin-1 (SIRT1) activator with an EC1.5 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].

SRT 1460 (2-6 μM; 72 hours) inhibits cell viability in a dose-dependent manner, with all pancreatic cancer cells being more sensitive than the control HPDE cell. The IC50s of those cells are: Patu8988t, 1.62±0.13 μM; SU86.86, 2.31±0.23 μM; Panc-1, 0.66 ±0.02 μM; HPDE, 2.39±0.29 μM[2].SRT 1460 (5 μM; 16 hours) increases expression of the autophagy marker LC3-II[2].

[1]. Milne JC, et al. Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes. Nature. 2007 Nov 29; 450(7170): 712-716.
[2]. Chini CC, et al. SIRT1-Activating Compounds (STAC) Negatively Regulate Pancreatic Cancer Cell Growth and Viability Through a SIRT1 Lysosomal-Dependent Pathway. Clin Cancer Res. 2016 May 15;22(10):2496-507.

Protocol:

SIRT1 2.9μM(EC1.5)