Thiomyristoyl是一种高效特异性SIRT2抑制剂,IC50值为28 nM。
产品描述
Thiomyristoyl is an effective and selective SIRT2 inhibitor (IC50: 28 nM). It inhibits SIRT1 (IC50: 98 μM) but no effect on SIRT3 even at 200 μM.
体外活性
在乳腺癌小鼠模型中,Thiomyristoyl可抑制SIRT2及肿瘤生长,并降低c-Myc蛋白水平.Thiomyristoyl的抗癌效应与c-Myc水平降低成正相关.
体内活性
Thiomyristoyl对SIRT3/5/6/7抑制效果很弱。Thiomyristoyl可降低体外癌症细胞中c-MYC的水平,在不同细胞系中其对c-MYC水平的降低程度与细胞系本身对Thiomyristoyl的敏感性成正比。
细胞实验
Human MCF-7 cells are grown in DMEM media contained 10% (vol/vol) heat-inactivated fetal bovine serum and 1% penicillin-streptomycin and treated with in the presence of 200 nM TSA for 6 hr. The acetylation level of p53 protein is determined by western blot using anti-acetyl-p53 (K382) antibody. β-actin serves as a loading control. (Only for Reference)
Cas No.
1429749-41-6
分子式
C34H51N3O3S
分子量
581.86
储存和溶解度
DMSO:100 mg/mL (171.87 mM)
Chloroform:Soluble
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years