Tenovin-1

目录号: GC14165纯度: >99.50%

A small molecule activator of p53

Cas No.: 380315-80-0

规格	价格	库存	数量
25mg	¥651.00	现货	1
50mg	¥1,323.00	现货	1
100mg	¥2,321.00	现货	1
10mM (in 1mL DMSO)	¥389.00	现货	1

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文献被引

本产品暂无引用记录;以下为 GlpBio 产品在 Nature / Cell / Science 等顶刊的客户引用样例

Nature
641, 529–536 (2025)
Nature
628, 630–638 (2024)
Nature
632, 686–694 (2024)
Nature
618, 1017–1023 (2023)
Nature
610, 366–372 (2022)
Cell
187(9):2288-2304 (2024)
Cell
183(7):1867-1883 (2020)
Science
388(6745) (2025)
Science
387(6739) (2025)
Science
387(6734) (2025)
Cell Research
35, 97–116 (2025)
Cell Research
34, 683–706 (2024)
Cell Research
33, 273–287 (2023)
Cell Research
33, 546–561 (2023)
Cell Research
33, 904–922 (2023)
Cell Research
31, 1291–1307 (2021)

产品描述 Description

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.

实验参考方法 Experimental Reference Method

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.
[2]. Yoon KB, et al. Induction of Nuclear Enlargement and Senescence by Sirtuin Inhibitors in Glioblastoma Cells. Immune Netw. 2016 Jun;16(3):183-8.
[3]. 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.
[4]. Grbesa I, et al. Expression of sirtuin 1 and 2 is associated with poor prognosis in non-small cell lung cancer patients. PLoS One. 2015 Apr 27;10(4):e0124670.
[5]. 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.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号

380315-80-0

化学名

N-[(4-acetamidophenyl)carbamothioyl]-4-tert-butylbenzamide

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 g/mol

溶解性

≥ 15 mg/mL in DMSO with gentle warming

保存条件

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°C，然后在超声波浴中震荡一段时间。

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。

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