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Sirt1 Inhibitor VII, Inauhzin-Calbiochem
| 产品编号： | 4169159 |
| 规格： | The Sirt1 Inhibitor VII, Inauhzin controls the biological activity of Sirt1. This small molecule/inhibitor is primarily used for Cell Structure applications. |
| 包装规格： | 10 MG |
| 产品类别： | 进口试剂 |
| 品牌： | Sigma-Aldrich |
| 优惠价： | 立即咨询 |
产品别名
Sirt1 Inhibitor VII, Inauhzin-Calbiochem
10-[2-(5H-[1,2,4]triazino[5,6-b]indol-3-ylthio)butanoyl]-10H-phenothiazine, INZ
基本信息
| Empirical Formula【经验(实验)分子式】 | C25H19N5OS2 |
| Molecular weight | 469.58 |
| General description【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 and effectively elevates cellular p53 lysine acetylation (Effective conc. 2 µM), thereby protecting p53 lysine residues from MDM2-mediated ubiquitination without directly inhibiting MDM2 function per se or its 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, 444151, & 444152) in blocking HCT116p53+/+ proliferation in vitro (by 29%, 76%, and >98, respectively, with 1 µM INZ alone, 4 µM Nutlin-3 alone, or in combination) and inducing HCT116p53+/+ apoptosis in mice in vivo (3.5% above control TUNEL staining with either drug treatment alone or 25% with combined treatment; 15 mg INZ/kg via daily i.p; 150 mg Nut-3/kg b.i.d. p.o.). 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, 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.). |
| Biochem/physiol Actions【生化/生理作用】 | Cell permeable: yes Reversible: yes |
| Warning【警告】 | Toxicity: Standard Handling (A) |
| Other Notes【其他说明】 | Zhang, Q., et al. 2012. EMBO Mol. Med.4, 298. Zhang, Y., et al. 2012. Cancer Biol. Ther.13, 915 |
| Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | powder |
| potency【效能】 | 0.7 μM IC50 |
| manufacturer/tradename | Calbiochem® |
| storage condition【储存条件】 | OK to freeze protect from light |
| color【颜色】 | beige |
| solubility【溶解性】 | DMSO: 100 mg/mL |
| shipped in【运输】 | wet ice |
| storage temp.【储存温度】 | 2-8℃ |
| packaging【包装】 | 10 mg in Glass bottle Packaged under inert gas |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
