2. Apoptosis
    Metabolic Enzyme/Protease
    Cell Cycle/DNA Damage
    Epigenetics
    Autophagy
  3. MDM-2/p53
    Dihydroorotate Dehydrogenase
    Sirtuin
    Autophagy
  4. Tenovin-1

Tenovin-1 

Cat. No.: HY-13423 Purity: 99.88%
COA Handling Instructions

Tenovin-1, a p53 activator, protects p53 from MDM2-mediated degradation. Tenovin-1 acts through inhibition of the protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 is also a dihydroorotate dehydrogenase (DHODH) inhibitor.

For research use only. We do not sell to patients.

Tenovin-1 Chemical Structure

Tenovin-1 Chemical Structure

CAS No. : 380315-80-0

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 165 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 165 In-stock
Solid
50 mg USD 150 In-stock
100 mg USD 273 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 3 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Tenovin-1, a p53 activator, protects p53 from MDM2-mediated degradation. Tenovin-1 acts through inhibition of the protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 is also a dihydroorotate dehydrogenase (DHODH) inhibitor[1][2].

IC50 & Target

MDM-2/p53

 

DHODH

 

Sirtuin

 

In Vitro

Tenovin-1 protects p53 from mdm2-mediated degradation with little effect on p53 synthesis. Tenovin-1 targets a factor(s) upstream of p53 that not only modulates p53 function but also other cellular pathways. Tenovin-1 (10 μM) inhibits SirT2 deacetylase activity[1].
Tenovin-1 (1-10 μM) induces a bell-shaped concentration-dependent cell death in SK-N-MC cells. Tenovin-1 alters the gene and protein expression of Bcl-2 family members. However, Tenovin-1 has a more powerful effect both on mRNA and protein expression levels at a lower concentration than does the higher concentration. Furthermore, Tenovin-1-induced cytotoxic effects depend on caspases in p53 wild-type WE-68 cells, but not in p53 null SK-N-MC cells. AIF plays a major role in tenovin-1-induced cell death in p53 null SK-N-MC cells, but not in p53 wild-type WE-68 cells. Reactive oxygen species are also involved in tenovin-1-mediated cell death in SK-N-MC cells. In addition, Tenovin-1 causes DNA damage in SK-N-MC cells[3]. Tenovin-1 (5 μM) increases the nuclear size in glioblastoma cells and rat primary astrocytes. Tenovin-1 induces cellular senescence, wich does not appear to be related to cell death[4].
Tenovin-1 (10 μM) reduces proliferation and anchorage independent growth of NSCLC cells. Tenovin-1 also inhibits cell growth of H358 lung cancer cells[5].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo

Tenovin-1 (92 mg/kg, i.p.) reduces growth of tumors in SCID mice derived from BL2 cells or ARN8 cells[5].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

369.48

Appearance

Solid

Formula

C20H23N3O2S
CAS No.
SMILES

O=C(NC(NC1=CC=C(NC(C)=O)C=C1)=S)C2=CC=C(C(C)(C)C)C=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (270.65 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.77 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.77 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.88%

COA (244 KB) LCMS (121 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[4]

Cell viability is measured by thiazolyl blue tetrazolium bromide (MTT) assay. Cells are seeded in 96-well plates. When indicated they are treated with 10 μM Tenovin-1 (tnv-1) or are transfected with siRNAs. After the specified period of time, MTT solution (0.5 mg/mL) is added. The formazan crystals are dissolved in an extraction buffer (50% dimethylformamide and 20% SDS, pH 4.7). The absorbance (540/690 nm) is measured in a SunRise plate reader[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[5]

ARN8 melanoma or BL2 Burkitt’s lymphoma cells are injected into the flank of SCID mice and allowed to develop until tumors become palpable. Tenovin-1 (in 70% cyclodextrin) is administered daily (14 days) by intraperitoneal injection at 92.5 mg/kg and tumor growth is measured over a period of 18 days. Control animals are treated with 70% cyclodextrin. In the BL2 experiment, n = 12 for each treatment. In the ARN8 experiment, n = 14 for the control group and n = 16 for the tenovin-1 treated group. Growth measurements are averaged between groups and plotted[5].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Tenovin-1380315-80-0Tenovin1Tenovin 1MDM-2/p53Dihydroorotate DehydrogenaseSirtuinAutophagyDHODHMDM2protein-deacetylatingacetylationdegradationInhibitorinhibitorinhibit

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