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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
Tenovin-6 Hydrochloride
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
1011301-29-3
- 规格：
1mg/5mg/2mg/10mg
| 规格： | 1mg | 产品价格： | ￥670.0 |
|---|---|---|---|
| 规格： | 5mg | 产品价格： | ￥2290.0 |
| 规格： | 2mg | 产品价格： | ￥1060.0 |
| 规格： | 10mg | 产品价格： | ￥3590.0 |
Tenovin-6是Tenovin-1的类似物，它抑制SIRT1，SIRT2和SIRT3的蛋白质脱乙酰基酶活性
| 基本信息 | |
| CAS | No.1011301-29-3 |
| 英文名称 | Tenovin-6 Hydrochloride |
| 分子式 | C25H35ClN4O2S |
| 分子量 | 491.09 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | Light yellow to yellow Solid |
| 储存条件 | Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| SMILES | O=C(NC(NC1=CC=C(NC(CCCCN(C)C)=O)C=C1)=S)C2=CC=C(C(C)(C)C)C=C2.Cl |
| 靶点 | Sirtuin |
| 通路 | Cell Cycle;DNA Damage/DNA Repair; Epigenetics |
| 背景说明 | Tenovin-6是Tenovin-1的类似物,它抑制SIRT1,SIRT2和SIRT3的蛋白质脱乙酰基酶活性。 |
| 生物活性 | Tenovin-6 Hydrochloride， an analog of Tenovin-1， is an activator of p53 transcriptional activity. Tenovin-6 Hydrochloride inhibits the protein deacetylase activities of purified human SIRT1， SIRT2， and SIRT3 with IC50s of 21 μM， 10 μM， and 67 μM， respectively. Tenovin-6 Hydrochloride also inhibits dihydroorotate dehydrogenase (DHODH)[1-2]. |
| In Vitro | Tenovin-6 Hydrochloride inhibits the growth of S. cerevisiae cultures with an IC50 of 30 μM and is more toxic to yeast than the less water-soluble tenovin-1. Tenovin-6 Hydrochloride rapidly increases the levels of endogenous K382-Ac p53 in MCF-7 cells[1]. |
| 细胞实验 | Tenovin-6 Hydrochloride(50 mg/kg，i.p.)inhibits the growth of tumor in mice[1]. |
| 动物实验 | Female SCID mice are injected subcutaneously with 1×106 ARN8 cells suspended in matrigel. Tumors are allowed to reach a size of approximately 10 mm3. Tenovin-6 is administered daily at 50 mg/kg by intraperitoneal injection. Control animals are treated with vehicle solution containing cyclodextrin 20%(w/v)and DMSO 10%(v/v). Tumor diameters are measured using calipers，and volumes are calculated using the equation V=π4/3[(d1 + d2)/4]3. Median values of tumor size are calculated for each time point as well as the corresponding 95% confidence intervals. Comparison of control and drug-treated tumor size distributions are made by Mann-Whitney U-test. An alpha-level of 0.05 is considered appropriate for determination of statistical significance.[1] |
| 激酶实验 | Assays are carried out using purified components in the Fluor de Lys Fluorescent Assay Systems. Relevant FdL substrates are used at 7 μM and NAD+ at 1 mM. Tenovins are solubilized in DMSO with the final DSMO concentration in the reaction being less than 0.25%. For SirT1 and HDAC8，one unit of enzyme is used per reaction，and for SirT2 and SirT3，five units is used per reaction. Reactions are carried out at 37°C for 1 hr.[1] |
| 数据来源文献 | [1]. Lain S， et al. Discovery， in vivo activity， and mechanism of action of a small-molecule p53 activator. Cancer Cell. 2008 May;13(5):454-63. [2]. Ladds MJGW， et al. Exploitation of DHODH and p53 activation as therapeutic targets - a case study in polypharmacology [published online ahead of print， 2020 Sep 8]. J Biol Chem. 2020;jbc.RA119.012056. |
| 单位 | 瓶 |
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IT1600 Tenovin-6 Hydrochloride 细胞周期 索莱宝
￥670 - 3590
