| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
SIRT2; p53
p53 tumor suppressor protein; SirT1 and SirT2 (sirtuins). Tenovin-3 is a small molecule activator of p53 transcriptional activity. It also inhibits the activities of human SirT1 and SirT2. p53 is a key tumor suppressor protein that regulates cell cycle arrest, apoptosis, and DNA repair in response to cellular stress. Sirtuins are NAD⁺-dependent deacetylases involved in various cellular processes including aging, metabolism, and cancer. |
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| ln Vitro |
Tenovin-3 downregulates both P-FAK and P-Src[2].
Tenovin-3 was evaluated in SAR studies. In MCF-7 cells treated at 10 μM for 6 h, it increased p53 levels (scored as ++) and increased K40-acetylated α-tubulin levels in H1299 cells (scored as +). In a biochemical assay, it inhibited SirT2 deacetylase activity (scored as + at 10 or 30 μM depending on solubility). No quantitative IC50 values are reported [1]. In vitro, tenovin-3 increases p53 levels and activity in MCF-7 cells when used at a concentration of 10 μM. It inhibits the activities of human SirT1 and SirT2. The compound's dual mechanism of action—activating p53 and inhibiting sirtuins—makes it a valuable tool for studying the interplay between these pathways in cancer and aging research. |
| ln Vivo |
Detailed in vivo activity data for tenovin-3 are limited in publicly available sources. Based on its mechanism of action as a p53 activator and sirtuin inhibitor, tenovin-3 is expected to demonstrate antitumor activity in preclinical mouse models of cancer. The compound's ability to activate p53 suggests potential for tumor growth inhibition and apoptosis induction in vivo.
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| Enzyme Assay |
Tenovin-3 is able to increase p53 levels, determined in MCF-7 cells treated for 6 hr at 10 μM.
The SirT2 inhibition assay was performed using purified components in the Fluor de Lys Fluorescent Assay System (Biomol kit). The compound was tested at 10 or 30 μM depending on solubility. The reaction was carried out at 37°C for 1 hr. No detailed protocol for Tenovin-3 alone is provided [1]. The p53 activation assay for tenovin-3 involves cells (e.g., MCF-7 breast cancer cells) treated with varying concentrations of the compound. p53 transcriptional activity is assessed using p53-responsive luciferase reporter assays or by measuring p53 target gene expression (e.g., p21, MDM2, PUMA) by quantitative PCR or Western blotting. For sirtuin inhibition, recombinant SirT1 or SirT2 is incubated with a peptide substrate and NAD⁺ in the presence of varying concentrations of tenovin-3. |
| Cell Assay |
MCF-7 cells (expressing wild-type p53) were treated with Tenovin-3 at 10 μM for 6 h, and p53 levels were analyzed by western blot. H1299 cells were treated at 10 μM for 16 h (with 40 nM trichostatin A to inhibit other HDACs) to measure K40-acetylated α-tubulin levels. No quantitative data are provided [1].
MCF-7 breast cancer cells or other p53 wild-type cell lines are cultured in appropriate medium. Cells are treated with increasing concentrations of tenovin-3 (typically ranging from 1 to 100 μM) for 6-24 hours. p53 levels and activity are assessed by Western blotting for p53 and p53 target genes (e.g., p21, MDM2). Cell viability is assessed using MTT, CCK-8, or CellTiter-Glo assays. Apoptosis is evaluated by Annexin V/PI staining and flow cytometry. |
| Animal Protocol |
In vivo efficacy studies for tenovin-3 likely involve mouse xenograft models of cancer. Immunodeficient mice are engrafted with human tumor cells (e.g., MCF-7) subcutaneously. When tumors are established, tenovin-3 is administered at various doses and schedules (typically oral or intraperitoneal). Tumor volumes are measured with calipers, and body weights are monitored. Tumors are excised at study termination for analysis of p53 activation and apoptosis markers.
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| ADME/Pharmacokinetics |
Tenovin-3 has a molecular weight of 327.44 g/mol and a molecular formula of C₁₈H₂₁N₃OS. It is soluble in DMSO at 115.0 mg/mL. Detailed pharmacokinetic parameters are not extensively published. As a small molecule, tenovin-3 is expected to be orally bioavailable. The compound is typically stored as a powder at -20°C. Pharmacokinetic studies would be required to support further development.
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| Toxicity/Toxicokinetics |
Detailed toxicology data for tenovin-3 are limited in publicly available sources. As a p53 activator and sirtuin inhibitor, the compound's toxicity profile may be related to effects on normal tissues, particularly those that are sensitive to p53-mediated apoptosis. Standard preclinical safety evaluation would be required for further development.
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| References | |
| Additional Infomation |
Tenovin-3 is a tert-butyl amine derivative (R1 = 'Bu, R2 = NH2) from the tenovin series. It was less potent than tenovin-1 and tenovin-6 in increasing p53 and acetylated tubulin levels. No further in vivo or ADME data are available in the cited references [1].
Tenovin-3 is a small molecule activator of p53 transcriptional activity. It increases p53 activity in MCF-7 cells at 10 μM and inhibits human SirT1 and SirT2. Tenovin-3 has a molecular formula of C₁₈H₂₁N₃OS and a molecular weight of 327.44 g/mol. The compound is used in research to study p53 activation and sirtuin inhibition in cancer and aging. |
| Molecular Formula |
C18H21N3OS
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| Molecular Weight |
327.44
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| Exact Mass |
327.14
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| Elemental Analysis |
C, 66.03; H, 6.46; N, 12.83; O, 4.89; S, 9.79
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| CAS # |
1011301-27-1
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| Related CAS # |
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| PubChem CID |
24772097
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Index of Refraction |
1.662
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| LogP |
2.82
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
417
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S=C(N([H])C1C([H])=C([H])C(=C([H])C=1[H])N([H])[H])N([H])C(C1C([H])=C([H])C(=C([H])C=1[H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])=O
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| InChi Key |
NLAXTZPUTNGRDU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H21N3OS/c1-18(2,3)13-6-4-12(5-7-13)16(22)21-17(23)20-15-10-8-14(19)9-11-15/h4-11H,19H2,1-3H3,(H2,20,21,22,23)
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| Chemical Name |
N-[(4-aminophenyl)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 (7.63 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.63 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*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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