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
• 经验公式（希尔记法）: C₂₅H₁₉N₅OS₂
• 分子量: 469.58
• UNSPSC代码: 12352200
• NACRES: NA.28

属性

• 质量水平: 100
• 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

说明

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

警告

Toxicity: Standard Handling (A)

其他说明

Zhang, Q., et al. 2012. EMBO Mol. Med.4, 298.
Zhang, Y., et al. 2012. Cancer Biol. Ther.13, 915

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全信息

• 储存分类代码: 11 - Combustible Solids
• WGK: WGK 3
• 闪点(°F): Not applicable
• 闪点(°C): Not applicable