566332
Sirt1 Inhibitor VII, Inauhzin
The Sirt1 Inhibitor VII, Inauhzin controls the biological activity of Sirt1. This small molecule/inhibitor is primarily used for Cell Structure applications.
别名:
Sirt1 Inhibitor VII, Inauhzin, 10-[2-(5H-[1,2,4]triazino[5,6-b]indol-3-ylthio)butanoyl]-10H-phenothiazine, INZ
质量水平
方案
≥98% (HPLC)
表单
powder
效能
0.7 μM IC50
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
beige
溶解性
DMSO: 100 mg/mL
运输
wet ice
储存温度
2-8°C
一般描述
A cell-permeable phenothiazine derivative that selectively inhibits SirT1 (IC50 ≤2.0 µM), but not SirT2, SirT3, or HCAC8 (IC50 >50 µM), activity. Effectively elevates cellular p53 lysine acetylation (Effective conc. 2 µM), thereby protecting p53 lysine residues from MDM2-mediated ubiquitination without inhibiting MDM2 activity toward deacetylated p53. Shown to inhibit cancer cell growth in a p53-dependent manner (IC50 = 2.0 and 15.7µM, respectively, against HCT116p53+/+ and HCT116p53-/- cells) and synergize with Nutlin-3 (Cat. Nos. 444143, https://www.sigmaaldrich.com/US/en/product/mm/444151" target="_blank"">444151, & 444152) in blocking HCT116p53+/+ proliferation in vitro (1 µM INZ & 4 µM Nutlin-3) and inducing HCT116p53+/+ apoptosis in mice in vivo (15 mg INZ/kg/d i.p; 150 mg Nut-3/kg/12 h p.o.).
生化/生理作用
Cell permeable: yes
Reversible: yes
包装
Packaged under inert gas
其他说明
Zhang, Q., et al. 2012. EMBO Mol. Med.4, 298.
Zhang, Y., et al. 2012. Cancer Biol. Ther.13, 915
Zhang, Y., et al. 2012. Cancer Biol. Ther.13, 915
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
Toxicity: Standard Handling (A)
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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