Tenovin-6 Hydrochloride
Based on 5 publication(s) in Google Scholar
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).
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- Pureza: 98.88%
- No. CAS: 1011301-29-3
- Fòrmula: C25H35ClN4O2S
- Peso molecular:491.09
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Tenovin-6 Hydrochloride
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Customer Validation & Images
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Cell Proliferation/Viability Assay
Actividad biológica
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SIRT2 10 μM (IC50) |
SIRT1 21 μM (IC50) |
SIRT3 67 μM (IC50) |
HDAC8 |
MDM-2/p53 |
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].
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 1011301-29-3
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Appearance Solid
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Peso molecular 491.09
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Fòrmula C25H35ClN4O2S
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Color Off-white to yellow
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SMILES
O=C(NC(NC1=CC=C(NC(CCCCN(C)C)=O)C=C1)=S)C2=CC=C(C(C)(C)C)C=C2.Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (5)
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Journal Impact Factor
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Most Recent
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Acta Pharmacol Sin
2022 Feb;43(2):457-469. PMID: 33850273 -
Lipids Health Dis
Elucidation of SIRT-1/PGC-1α-associated mitochondrial dysfunction and autophagy in nonalcoholic fatty liver disease. [Abstract]2021 Apr 26;20(1):40. PMID: 33902605 -
J Nutr
A-Type Cinnamon Procyanidin Oligomers Protect Against 1-Methyl-4-Phenyl-1,2,3,6-Tetrahydropyridine-Induced Neurotoxicity in Mice Through Inhibiting the P38 Mitogen-Activated Protein Kinase/P53/BCL-2 Associated X Protein Signaling Pathway. [Abstract]2020 Jul 1;150(7):1731-1737. PMID: 32386222
Tenovin-6 Hydrochloride purchased from MedChemExpress. Usage Cited in: J Nutr. 2020 Jul 1;150(7):1731-1737. [Abstract]
The cell viability in untreated SH-SY5Y cells or those stimulated with Tenovin-6 and then treated with MPP+ or the combination of MPP+ and CPO-A.
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Exp Cell Res
Tenovin-6 induces the SIRT-independent cell growth suppression and blocks autophagy flux in canine hemangiosarcoma cell lines. [Abstract]2020 Mar 1;388(1):111810. PMID: 31891684 -
Solvente y solubilidad
DMSO : ≥ 49 mg/mL (99.78 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocolo
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
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 (279 KB)
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SDS (641 KB)
- English - EN (641 KB)
- Français - FR (641 KB)
- Deutsch - DE (641 KB)
- Norwegian - NO (641 KB)
- Español - ES (641 KB)
- Swedish - SV (641 KB)
- Italian - IT (641 KB)
- Korean - KR (641 KB)
- Portuguese - PT (641 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 May;13(5):454-63. [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]. 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. [Content Brief]
[4]. Yuan H, et al. Tenovin-6 impairs autophagy by inhibiting autophagic flux. Cell Death Dis. 2017 Feb 9;8(2):e2608. [Content Brief]
[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. [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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0363 mL | 10.1814 mL | 20.3629 mL | 50.9072 mL |
| 5 mM | 0.4073 mL | 2.0363 mL | 4.0726 mL | 10.1814 mL | |
| 10 mM | 0.2036 mL | 1.0181 mL | 2.0363 mL | 5.0907 mL | |
| 15 mM | 0.1358 mL | 0.6788 mL | 1.3575 mL | 3.3938 mL | |
| 20 mM | 0.1018 mL | 0.5091 mL | 1.0181 mL | 2.5454 mL | |
| 25 mM | 0.0815 mL | 0.4073 mL | 0.8145 mL | 2.0363 mL | |
| 30 mM | 0.0679 mL | 0.3394 mL | 0.6788 mL | 1.6969 mL | |
| 40 mM | 0.0509 mL | 0.2545 mL | 0.5091 mL | 1.2727 mL | |
| 50 mM | 0.0407 mL | 0.2036 mL | 0.4073 mL | 1.0181 mL | |
| 60 mM | 0.0339 mL | 0.1697 mL | 0.3394 mL | 0.8485 mL | |
| 80 mM | 0.0255 mL | 0.1273 mL | 0.2545 mL | 0.6363 mL |
Tenovin-6 Hydrochloride Related Classifications
HY-15510B Related Classifications
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