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Chemical Structure| 1011557-82-6 Chemical Structure| 1011557-82-6

Structure of Tenovin-6
CAS No.: 1011557-82-6

Chemical Structure| 1011557-82-6

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Tenovin-6 is the water soluble analog of Tenovin-1 and acts as a potent SIRT1 (IC50=21 μM) and SIRT2 (IC50= 10 μM) inhibitor as well as p53 activator.

Synonyms: Tenovin-6

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Product Details of Tenovin-6

CAS No. :1011557-82-6
Formula : C25H34N4O2S
M.W : 454.63
SMILES Code : O=C(NC(NC1=CC=C(NC(CCCCN(C)C)=O)C=C1)=S)C2=CC=C(C(C)(C)C)C=C2
Synonyms :
Tenovin-6
MDL No. :MFCD11976906
InChI Key :BVJSXSQRIUSRCO-UHFFFAOYSA-N
Pubchem ID :24772043

Safety of Tenovin-6

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Tenovin-6

epigenetics

Isoform Comparison

Biological Activity

Description
Tenovin-6, an analog of Tenovin-1, is an activator of p53 transcriptional activity. Tenovin-6 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 also inhibits dihydroorotate dehydrogenase (DHODH)[1].[2].
Target
  • SIRT1

    SIRT1, IC50:21 μM

  • SIRT2

    SIRT2, IC50:10 μM

  • SIRT3

    SIRT3, IC50:67 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
Myeloma cells (U266) 4 μM 24 h Tenovin-6 had minimal effects on the proliferation of U266 cells. J Pathol. 2017 Jul;242(3):309-321.
human hepatocarcinoma cell line Huh7 5 μM 24 h Tenovin-6 treatment significantly increased LC3B-II levels in Huh7 cells, and this increase was dose-dependent. Cell Death Dis. 2017 Feb 9;8(2):e2608.
human lung adenocarcinoma epithelial cell line A549 10 μM 24 h Tenovin-6 treatment significantly increased LC3B-II levels in A549 cells, and this increase was dose-dependent. Cell Death Dis. 2017 Feb 9;8(2):e2608.
mouse embryonic fibroblasts (MEFs) 5 μM 24 h Tenovin-6 significantly increased LC3A/B-II levels in wild-type MEF cells but not in ATG5−/− and ATG7−/− MEF cells. Cell Death Dis. 2017 Feb 9;8(2):e2608.
chronic lymphocytic leukaemia (CLL) cell 10 µM 24 h To investigate the cytotoxic effect of Tenovin-6 on CLL cells, results showed that Tenovin-6 induced cell death without significant apoptotic features, and a significant increase in autophagosome number was observed. Br J Cancer. 2013 Oct 29;109(9):2434-44.
chronic lymphocytic leukaemia (CLL) cell 10 µM 4 h To investigate the effect of Tenovin-6 on autophagy regulation in CLL cells, results showed that Tenovin-6 inhibited autophagy, leading to an increase in autophagosome number and accumulation of LC3 II and p62/Sequestosome 1. Br J Cancer. 2013 Oct 29;109(9):2434-44.
Burkitt’s lymphoma cells (BJAB) 4 μM 24 h Tenovin-6 had minimal effects on the proliferation of BJAB cells. J Pathol. 2017 Jul;242(3):309-321.
PEL cells (BC3, BCBL-1, BCP1, JSC1) 4 μM 24 h Tenovin-6 inhibited the proliferation of PEL cells, induced cell cycle arrest and apoptosis. J Pathol. 2017 Jul;242(3):309-321.
chronic lymphocytic leukemia cells 10 µM 4 h or 24 h To investigate the effects of Tenovin-6 on CLL cells, it was found to cause cell death through autophagy inhibition rather than inducing apoptosis via the p53 pathway. Br J Cancer. 2013 Oct 29;109(9):2434-44.
H1650 cells 10 μM 48 h Tenovin-6 in combination with metformin significantly inhibited cell growth. J Cell Mol Med. 2019 Apr;23(4):2872-2889.
H460 cells 10 μM 48 h Tenovin-6 in combination with metformin significantly inhibited cell growth. J Cell Mol Med. 2019 Apr;23(4):2872-2889.
H1299 cells 10 μM 48 h Tenovin-6 in combination with metformin significantly inhibited cell growth. J Cell Mol Med. 2019 Apr;23(4):2872-2889.
A549 cells 10 μM 48 h Tenovin-6 in combination with metformin inhibited cell proliferation more effectively than either agent alone. J Cell Mol Med. 2019 Apr;23(4):2872-2889.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NOD/SCID mice PEL model Intraperitoneal injection 50 mg/kg Daily until the end of the experiment Tenovin-6 significantly inhibited the initiation and progression of PEL and extended the survival of mice. J Pathol. 2017 Jul;242(3):309-321.
NSG mice Patient-derived xenograft model Intraperitoneal injection 50 mg/kg Twice daily for 3 weeks Combination therapy of TV-6 with gefitinib significantly inhibited tumor growth and prolonged remission Neoplasia. 2020 Jan;22(1):33-46

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.20mL

0.44mL

0.22mL

11.00mL

2.20mL

1.10mL

22.00mL

4.40mL

2.20mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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