Tenovin-1
Based on 5 publication(s) in Google Scholar
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.
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- Pureza: 99.88%
- No. CAS: 380315-80-0
- Fòrmula: C20H23N3O2S
- Peso molecular:369.48
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
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Publications Citing Use of MedChemExpress (MCE) Tenovin-1
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Actividad biológica
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MDM-2/p53 |
DHODH |
Sirtuin |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDCK | CC50 |
50 μM
Compound: 8j
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Cytotoxicity against MDCK cells by CCK-8 assay
Cytotoxicity against MDCK cells by CCK-8 assay
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[PMID: 37531746] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 380315-80-0
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Appearance Solid
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Peso molecular 369.48
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Fòrmula C20H23N3O2S
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Color White to off-white
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SMILES
O=C(NC(NC1=CC=C(NC(C)=O)C=C1)=S)C2=CC=C(C(C)(C)C)C=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
DMSO : 100 mg/mL (270.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.77 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7065 mL | 13.5325 mL | 27.0651 mL | 67.6627 mL |
| 5 mM | 0.5413 mL | 2.7065 mL | 5.4130 mL | 13.5325 mL | |
| 10 mM | 0.2707 mL | 1.3533 mL | 2.7065 mL | 6.7663 mL | |
| 15 mM | 0.1804 mL | 0.9022 mL | 1.8043 mL | 4.5108 mL | |
| 20 mM | 0.1353 mL | 0.6766 mL | 1.3533 mL | 3.3831 mL | |
| 25 mM | 0.1083 mL | 0.5413 mL | 1.0826 mL | 2.7065 mL | |
| 30 mM | 0.0902 mL | 0.4511 mL | 0.9022 mL | 2.2554 mL | |
| 40 mM | 0.0677 mL | 0.3383 mL | 0.6766 mL | 1.6916 mL | |
| 50 mM | 0.0541 mL | 0.2707 mL | 0.5413 mL | 1.3533 mL | |
| 60 mM | 0.0451 mL | 0.2255 mL | 0.4511 mL | 1.1277 mL | |
| 80 mM | 0.0338 mL | 0.1692 mL | 0.3383 mL | 0.8458 mL | |
| 100 mM | 0.0271 mL | 0.1353 mL | 0.2707 mL | 0.6766 mL |
Tenovin-1 Related Classifications
HY-13423 Related Classifications
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