标签归档：tenovin

Tenovin-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Tenovin-1  纯度: 99.88%

Tenovin-1 是 sirtuin 1 和 sirtuin 2 的抑制剂，同时可激活 p53，具有潜在的癌症研究的潜力。

Tenovin-1

Tenovin-1 Chemical Structure

CAS No. : 380315-80-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1500 In-stock
50 mg ￥1360 In-stock
100 mg ￥2480 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Tenovin-1 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Epigenetics Compound Library
  • Metabolism/Protease Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Antioxidants Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Ferroptosis Compound Library
  • Pyroptosis Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Mitochondria-Targeted Compound Library
  • Transcription Factor Targeted Library
  • Anti-Colorectal Cancer Compound Library

生物活性

Tenovin-1, a p53 activator, protects p53 from MDM2-mediated degradation. Tenovin-1 acts through inhibition of the protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 is also a dihydroorotate dehydrogenase (DHODH) inhibitor[1][2].

IC50 & Target

Sirtuin

 

MDM-2/p53

 

DHODH

 

体外研究
(In Vitro)

Tenovin-1 protects p53 from mdm2-mediated degradation with little effect on p53 synthesis. Tenovin-1 targets a factor(s) upstream of p53 that not only modulates p53 function but also other cellular pathways. Tenovin-1 (10 μM) inhibits SirT2 deacetylase activity[1].
Tenovin-1 (1-10 μM) induces a bell-shaped concentration-dependent cell death in SK-N-MC cells. Tenovin-1 alters the gene and protein expression of Bcl-2 family members. However, Tenovin-1 has a more powerful effect both on mRNA and protein expression levels at a lower concentration than does the higher concentration. Furthermore, Tenovin-1-induced cytotoxic effects depend on caspases in p53 wild-type WE-68 cells, but not in p53 null SK-N-MC cells. AIF plays a major role in tenovin-1-induced cell death in p53 null SK-N-MC cells, but not in p53 wild-type WE-68 cells. Reactive oxygen species are also involved in tenovin-1-mediated cell death in SK-N-MC cells. In addition, Tenovin-1 causes DNA damage in SK-N-MC cells[3]. Tenovin-1 (5 μM) increases the nuclear size in glioblastoma cells and rat primary astrocytes. Tenovin-1 induces cellular senescence, wich does not appear to be related to cell death[4].
Tenovin-1 (10 μM) reduces proliferation and anchorage independent growth of NSCLC cells. Tenovin-1 also inhibits cell growth of H358 lung cancer cells[5].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Tenovin-1 (92 mg/kg, i.p.) reduces growth of tumors in SCID mice derived from BL2 cells or ARN8 cells[5].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

369.48

Formula

C20H23N3O2S
CAS 号

380315-80-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (270.65 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7065 mL 13.5325 mL 27.0651 mL
5 mM 0.5413 mL 2.7065 mL 5.4130 mL
10 mM 0.2707 mL 1.3533 mL 2.7065 mL

*

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.77 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.77 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.77 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.77 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Lain S, et al. Discovery, in vivo activity, and mechanism of action of a small-molecule p53 activator. Cancer Cell. 2008;13(5):454-463.

    [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.

    [3]. 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.

    [4]. Yoon KB, et al. Induction of Nuclear Enlargement and Senescence by Sirtuin Inhibitors in Glioblastoma Cells. Immune Netw. 2016 Jun;16(3):183-8.

    [5]. 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.
Cell Assay
[4]

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[5]

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Lain S, et al. Discovery, in vivo activity, and mechanism of action of a small-molecule p53 activator. Cancer Cell. 2008;13(5):454-463.

    [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.

    [3]. 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.

    [4]. Yoon KB, et al. Induction of Nuclear Enlargement and Senescence by Sirtuin Inhibitors in Glioblastoma Cells. Immune Netw. 2016 Jun;16(3):183-8.

    [5]. 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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

生物活性分子抑制剂Tenovin-6

发表于由

生物活性分子抑制剂 特异性抑制剂 激动剂 化合物库 重组蛋白 Tenovin-6  纯度: 98.67%

Tenovin-6 是 Tenovin-1 (HY-13423) 的类似物，是一种 p53 转录活性的激活剂。Tenovin-6 Hydrochloride 抑制纯化人 SIRT1、SIRT2 和 SIRT3 蛋白脱乙酰酶活性，IC50 分别为 21 μM、10 μM 和 67 μM。Tenovin-6 也能抑制二氢乳清酸脱氢酶 (DHODH)。

Tenovin-6

Tenovin-6 Chemical Structure

CAS No. : 1011557-82-6

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥2300 In-stock
2 mg ￥990 In-stock
5 mg ￥2300 In-stock
10 mg ￥3600 In-stock
50 mg ￥9900 In-stock
100 mg 询价

* Please select Quantity before adding items.

Tenovin-6 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Epigenetics Compound Library
  • Metabolism/Protease Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Antioxidants Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Ferroptosis Compound Library
  • Pyroptosis Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Mitochondria-Targeted Compound Library
  • Transcription Factor Targeted Library
  • Anti-Colorectal Cancer Compound Library

生物活性

Tenovin-6, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 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 also inhibits dihydroorotate dehydrogenase (DHODH)[1][2].

IC50 & Target[1]

SIRT2

10 μM (IC50)

SIRT1

21 μM (IC50)

SIRT3

67 μM (IC50)

HDAC8

 

MDM-2/p53

 

体外研究
(In Vitro)

Tenovin-6 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 rapidly increases the levels of endogenous K382-Ac p53 in MCF-7 cells[1].
Tenovin-6 (0 to 15 μM) dose dependently increases the level of LC3-II in diverse cell types, and the increase is ATG5/7 dependent. Tenovin-6 treatment also increases the number and intensity of autophagic vesicles with or without the presence of Torin 1, and prevents Torin 1-induced SQSTM1/p62 degradation. Tenovin-6 affects the acidification of autolysosomes and impairs the hydrolytic activity of lysosomes but does not affect the fusion between autophagosomes and lysosomes. That tenovin-6 inhibits autophagy does not correlate with p53 activation and SIRT1/2 inhibition by knockdown or knockout cannot mimic the effect of tenovin-6 on LC3B accumulation[3].
Tenovin-6 (0, 1, 2.5, 5 or 10 μM) potently inhibits cell proliferation in a dose- and time-dependent manner in all OCI-Ly1, DHL-10, U2932, RIVA, HBL1 and OCI-Ly10 cell lines. Tenovin-6 consistently increases LC3B-II level in DLBCL cell lines by inhibiting the classical autophagy pathway, without activating p53, and the increase is independent of SIRT1/2/3 and p53. Tenovin-6 induces apoptosis through the extrinsic cell-death pathway[4.
Tenovin-6 suppresses the growth of UM cells with IC50 of 12.8 μM, 11.0 μM, 14.58 μM and 9.62 μM for 92.1, Mel 270, Omm 1 and Omm 2.3 cells, respectively[5].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Tenovin-6 (50 mg/kg, i.p.) inhibits the growth of tumor in mice[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

454.63

Formula

C25H34N4O2S
CAS 号

1011557-82-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 31 mg/mL (68.19 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1996 mL 10.9980 mL 21.9959 mL
5 mM 0.4399 mL 2.1996 mL 4.3992 mL
10 mM 0.2200 mL 1.0998 mL 2.1996 mL

*

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.50 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.50 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [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.

    [3]. Dai W, et al. Class III-specific HDAC inhibitor Tenovin-6 induces apoptosis, suppresses migration and eliminates cancer stem cells in uveal melanoma. Sci Rep. 2016 Mar 4;6:22622.

    [4]. Yuan H, et al. Tenovin-6 impairs autophagy by inhibiting autophagic flux. Cell Death Dis. 2017 Feb 9;8(2):e2608.

    [5]. Yuan H, et al. Tenovin-6 inhibits proliferation and survival of diffuse large B-cell lymphoma cells by blocking autophagy. Oncotarget. 2017 Feb 28;8(9):14912-14924.
Kinase Assay
[1]

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.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[4]

The MTS assay is used to evaluate cell viability. UM cells are seeded into each well of 96-well plates (5,000 cells/well) and treated the next day with control or Tenovin-6 in an increasing concentrations from 0 to 20 μM for 68 h, and then MTS is added at 20 μL/well to be read at a wave length of 490 nm, the IC50 is determined by curve fitting of the sigmoidal dose-response curve.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

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.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [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.

    [3]. Dai W, et al. Class III-specific HDAC inhibitor Tenovin-6 induces apoptosis, suppresses migration and eliminates cancer stem cells in uveal melanoma. Sci Rep. 2016 Mar 4;6:22622.

    [4]. Yuan H, et al. Tenovin-6 impairs autophagy by inhibiting autophagic flux. Cell Death Dis. 2017 Feb 9;8(2):e2608.

    [5]. Yuan H, et al. Tenovin-6 inhibits proliferation and survival of diffuse large B-cell lymphoma cells by blocking autophagy. Oncotarget. 2017 Feb 28;8(9):14912-14924.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Tenovin-3

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Tenovin-3  纯度: 99.86%

Tenovin-3 是p53 的激活剂。

Tenovin-3

Tenovin-3 Chemical Structure

CAS No. : 1011301-27-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1333 In-stock
1 mg ￥900 In-stock
5 mg ￥1850 In-stock
10 mg ￥3100 In-stock
25 mg ￥6600 In-stock
50 mg ￥11000 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Tenovin-3 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Ferroptosis Compound Library
  • Pyroptosis Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Transcription Factor Targeted Library
  • Anti-Colorectal Cancer Compound Library

生物活性

Tenovin-3 is a p53 activator[1][2].

体外研究
(In Vitro)

Tenovin-3 downregulates both P-FAK and P-Src[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

327.44

Formula

C18H21N3OS
CAS 号

1011301-27-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 31 mg/mL (94.67 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0540 mL 15.2700 mL 30.5399 mL
5 mM 0.6108 mL 3.0540 mL 6.1080 mL
10 mM 0.3054 mL 1.5270 mL 3.0540 mL

*

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.63 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.63 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.63 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.63 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [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]. Jifei Miao, et al. Nuclear HMGB1 promotes the phagocytic ability of macrophages. Exp Cell Res. 2020 Aug 1;393(1):112037.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Tenovin-6 Hydrochloride

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Tenovin-6 Hydrochloride  纯度: ≥98.0%

Tenovin-6 Hydrochloride 是 Tenovin-1 (HY-13423) 的类似物，是一种 p53 转录活性的激活剂。Tenovin-6 Hydrochloride 抑制纯化人 SIRT1、SIRT2 和 SIRT3 蛋白脱乙酰酶活性，IC50 分别为 21 μM、10 μM 和 67 μM。Tenovin-6 Hydrochloride 也能抑制二氢乳清酸脱氢酶 (DHODH)。

Tenovin-6 Hydrochloride

Tenovin-6 Hydrochloride Chemical Structure

CAS No. : 1011301-29-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2485 In-stock
2 mg ￥990 In-stock
5 mg ￥2300 In-stock
10 mg ￥3600 In-stock
50 mg ￥9900 In-stock
100 mg 询价

* Please select Quantity before adding items.

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生物活性

Tenovin-6 Hydrochloride, an analog of Tenovin-1 (HY-13423), 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].

IC50 & Target[1]

SIRT2

10 μM (IC50)

SIRT1

21 μM (IC50)

SIRT3

67 μM (IC50)

HDAC8

 

MDM-2/p53

 

体外研究
(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].
Tenovin-6 Hydrochloride (0 to 15 μM) dose dependently increases the level of LC3-II in diverse cell types, and the increase is ATG5/7 dependent. Tenovin-6 Hydrochloride treatment also increases the number and intensity of autophagic vesicles with or without the presence of Torin 1, and prevents Torin 1-induced SQSTM1/p62 degradation. Tenovin-6 Hydrochloride affects the acidification of autolysosomes and impairs the hydrolytic activity of lysosomes but does not affect the fusion between autophagosomes and lysosomes. That Tenovin-6 Hydrochloride inhibits autophagy does not correlate with p53 activation and SIRT1/2 inhibition by knockdown or knockout cannot mimic the effect of Tenovin-6 Hydrochloride on LC3B accumulation[3].
Tenovin-6 Hydrochloride (0, 1, 2.5, 5 or 10 μM) potently inhibits cell proliferation in a dose- and time-dependent manner in all OCI-Ly1, DHL-10, U2932, RIVA, HBL1 and OCI-Ly10 cell lines. Tenovin-6 Hydrochloride consistently increases LC3B-II level in DLBCL cell lines by inhibiting the classical autophagy pathway, without activating p53, and the increase is independent of SIRT1/2/3 and p53. Tenovin-6 Hydrochloride induces apoptosis through the extrinsic cell-death pathway[4.
Tenovin-6 Hydrochloride suppresses the growth of UM cells with IC50 of 12.8 μM, 11.0 μM, 14.58 μM and 9.62 μM for 92.1, Mel 270, Omm 1 and Omm 2.3 cells, respectively[5].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Tenovin-6 Hydrochloride (50 mg/kg, i.p.) inhibits the growth of tumor in mice[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

491.09

Formula

C25H35ClN4O2S
CAS 号

1011301-29-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : ≥ 49 mg/mL (99.78 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0363 mL 10.1814 mL 20.3629 mL
5 mM 0.4073 mL 2.0363 mL 4.0726 mL
10 mM 0.2036 mL 1.0181 mL 2.0363 mL

*

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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。
参考文献

  • [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.

    [3]. Dai W, et al. Class III-specific HDAC inhibitor Tenovin-6 induces apoptosis, suppresses migration and eliminates cancer stem cells in uveal melanoma. Sci Rep. 2016 Mar 4;6:22622.

    [4]. Yuan H, et al. Tenovin-6 impairs autophagy by inhibiting autophagic flux. Cell Death Dis. 2017 Feb 9;8(2):e2608.

    [5]. Yuan H, et al. Tenovin-6 inhibits proliferation and survival of diffuse large B-cell lymphoma cells by blocking autophagy. Oncotarget. 2017 Feb 28;8(9):14912-14924.
Kinase Assay
[1]

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.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[4]

The MTS assay is used to evaluate cell viability. UM cells are seeded into each well of 96-well plates (5,000 cells/well) and treated the next day with control or Tenovin-6 in an increasing concentrations from 0 to 20 μM for 68 h, and then MTS is added at 20 μL/well to be read at a wave length of 490 nm, the IC50 is determined by curve fitting of the sigmoidal dose-response curve.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

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.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [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.

    [3]. Dai W, et al. Class III-specific HDAC inhibitor Tenovin-6 induces apoptosis, suppresses migration and eliminates cancer stem cells in uveal melanoma. Sci Rep. 2016 Mar 4;6:22622.

    [4]. Yuan H, et al. Tenovin-6 impairs autophagy by inhibiting autophagic flux. Cell Death Dis. 2017 Feb 9;8(2):e2608.

    [5]. Yuan H, et al. Tenovin-6 inhibits proliferation and survival of diffuse large B-cell lymphoma cells by blocking autophagy. Oncotarget. 2017 Feb 28;8(9):14912-14924.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务