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Purity: ≥98%
Tenovin-1 is a novel and potent activator of p53 that guards against MDM2-mediated p53 degradation. It was discovered by a cell-based screen. It works by preventing SirT1 and SirT2 from deacetylating proteins, increasing levels of the p53 protein, p21CIP/WAF1 protein, and mRNA, and protecting p53 from mdm2-mediated degradation with little effect on p53 synthesis.
| Targets |
Sirtuin; MDM-2/p53; DHODH
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| ln Vitro |
Tenovin-1 is a p53 activator and elevates the amount of p53 protein within 2 hr of treatment. Treatment with tenovin-1 has no effect on the levels of p53 mRNA. With little impact on p53 synthesis, tenovin-1 (10μM) defends p53 from mdm2-mediated degradation. In a panel of tumor cells expressing p53, tenovin-1 inhibits cell growth and triggers apoptosis. Tenovin-1 functions by preventing SirT1 and SirT2, two significant sirtuin family members, from deacetylating proteins. [1]
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| ln Vivo |
Tenovin-1 inhibits the growth of tumor xenografts derived from BL2, according to early in vivo experiments. [1]
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| Cell Assay |
Thiazolyl blue tetrazolium bromide (MTT) assay is used to determine cell viability. In 96-well plates, cells are sown. When indicated, they receive a siRNA transfection or 10 μM Tenovin-1 (tnv-1) treatment. MTT solution (0.5 mg/mL) is added after the allotted amount of time has passed. In an extraction buffer (50% dimethylformamide and 20% SDS, pH 4.7) the formazan crystals are dissolved. A SunRise plate reader is used to measure the absorbance (540–690 nm).
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| References |
| Molecular Formula |
C20H23N3O2S
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| Molecular Weight |
369.48
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| Exact Mass |
369.15
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| Elemental Analysis |
C, 65.01; H, 6.27; N, 11.37; O, 8.66; S, 8.68
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| CAS # |
380315-80-0
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
CC(=O)NC1=CC=C(C=C1)NC(=S)NC(=O)C2=CC=C(C=C2)C(C)(C)C
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| InChi Key |
WOWJIWFCOPZFGV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H23N3O2S/c1-13(24)21-16-9-11-17(12-10-16)22-19(26)23-18(25)14-5-7-15(8-6-14)20(2,3)4/h5-12H,1-4H3,(H,21,24)(H2,22,23,25,26)
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| Chemical Name |
N-[(4-acetamidophenyl)carbamothioyl]-4-tert-butylbenzamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.77 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.77 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 15% Captisol: 15 mg/mL |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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