| 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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| 250mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
SIRT2; p53
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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]. |
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| ln 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]. |
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| 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].
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| Animal Protocol |
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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].
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| 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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