Tenovin-1
目录号 : GC14165
A small molecule activator of p53
Cas No.:380315-80-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | Cell viability is measured by thiazolyl blue tetrazolium bromide (MTT) assay. Cells are seeded in 96-well plates. When indicated they are treated with 10 μM Tenovin-1 (tnv-1) or are transfected with siRNAs. After the specified period of time, MTT solution (0.5 mg/mL) is added. The formazan crystals are dissolved in an extraction buffer (50% dimethylformamide and 20% SDS, pH 4.7). The absorbance (540/690 nm) is measured in a SunRise plate reader[4]. |
Animal experiment: | ARN8 melanoma or BL2 Burkitt’s lymphoma cells are injected into the flank of SCID mice and allowed to develop until tumors become palpable. Tenovin-1 (in 70% cyclodextrin) is administered daily (14 days) by intraperitoneal injection at 92.5 mg/kg and tumor growth is measured over a period of 18 days. Control animals are treated with 70% cyclodextrin. In the BL2 experiment, n = 12 for each treatment. In the ARN8 experiment, n = 14 for the control group and n = 16 for the tenovin-1 treated group. Growth measurements are averaged between groups and plotted[5]. |
References: [1]. Marx C, et al. The sirtuin 1/2 inhibitor tenovin-1 induces a nonlinear apoptosis-inducing factor-dependent cell death in a p53 null Ewing's sarcoma cell line. Invest New Drugs. 2017 Nov 18. | |
Tenovin-1, a small molecule discovered by a cell-based screen, is a bio-active activator of p53 that elevates the levels of p53 protein, p53-downstream target p21CIP/WAF1 protein and mRNA and protects p53 from mdm2-mediated degradation with little impact on p53 synthesis. Tenovin-1 also exerts inhibition against human sirtuin 1 (SirT1) and sirtuin 2 (SirT2), two important members of the sirtuin family. Due to its insufficient solubility, an improved and water-soluble version of tenovin-1 has been found to decrease the peptide deacetylase activity of human SirT1 and SirT2 with values of 50% inhibition concentration IC50 of 21 μM and 10 μM respectively.
Reference
[1].Lain S, Hollick JJ, Campbell J, Staples OD, Higgins M, Aoubala M, McCarthy A, Appleyard V, Murray KE, Baker L, Thompson A, Mathers J, Holland SJ, Stark MJ, Pass G, Woods J, Lane DP, Westwood NJ. Discovery, in vivo activity, and mechanism of action of a small-molecule p53 activator. Cancer Cell. 2008 May;13(5):454-63. doi: 10.1016/j.ccr.2008.03.004.
| Cas No. | 380315-80-0 | SDF | |
| 化学名 | N-[(4-acetamidophenyl)carbamothioyl]-4-tert-butylbenzamide | ||
| Canonical SMILES | CC(=O)NC1=CC=C(C=C1)NC(=S)NC(=O)C2=CC=C(C=C2)C(C)(C)C | ||
| 分子式 | C20H23N3O2S | 分子量 | 369.5 |
| 溶解度 | ≥ 15 mg/mL in DMSO with gentle warming | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7064 mL | 13.5318 mL | 27.0636 mL |
| 5 mM | 0.5413 mL | 2.7064 mL | 5.4127 mL |
| 10 mM | 0.2706 mL | 1.3532 mL | 2.7064 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。