半岛bd体育手机客户端 说明
一般描述
A cell-permeable phenothiazine derivative that selectively inhibits SirT1 (IC50≤2.0 ?M), but not SirT2, SirT3, or HCAC8 (IC50>50 ?M), activity and effectively elevates cellular p53 lysine acetylation (Effective conc. 2 ?M), 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 15.7?M, respectively, against HCT116p53+/+and HCT116p53-/-cells) and synergize with Nutlin-3 (Cat. Nos. 444143, 444151, & 444152) in blocking HCT116p53+/+proliferationin vitro(by 29%, 76%, and >98, respectively, with 1 ?M INZ alone, 4 ?M Nutlin-3 alone, or in combination) and inducing HCT116p53+/+apoptosis in micein 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 ?M), but not SirT2, SirT3, or HCAC8 (IC50>50 ?M), activity. Effectively elevates cellular p53 lysine acetylation (Effective conc. 2 ?M), 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 15.7?M, respectively, against HCT116p53+/+and HCT116p53-/-cells) and synergize with Nutlin-3 (Cat. Nos. 444143, 444151, & 444152) in blocking HCT116p53+/+proliferationin vitro(1 ?M INZ & 4 ?M Nutlin-3) and inducing HCT116p53+/+apoptosis in micein vivo(15 mg INZ/kg/d i.p; 150 mg Nut-3/kg/12 h p.o.).
包装
10 mg in Glass bottle
Packaged under inert gas
生化/生理作用
Cell permeable: yes
Reversible: yes
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
基本信息
| 经验(实验)分子式 | C25H19N5OS2 |
| 分子量 | 469.58 |
半岛bd体育手机客户端 性质
| 质量水平 | 100 |
| 测定 | ≥98% (HPLC) |
| 形式 | powder |
| 效能 | 0.7 μM IC50 |
| manufacturer/tradename | 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℃ |
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 |
Sigma-Aldrich
m.cnreagent.com
