Tenovin-1

Catalog No.S8000

For research use only.

Tenovin-1 protects against MDM2-mediated p53 degradation, which involves ubiquitination, and acts through inhibition of protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 is also an inhibitor of dihydroorotate dehydrogenase (DHODH).

Tenovin-1 Chemical Structure

CAS No. 380315-80-0

Selleck's Tenovin-1 has been cited by 5 Publications

1 Customer Review

Purity & Quality Control

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Biological Activity

Description Tenovin-1 protects against MDM2-mediated p53 degradation, which involves ubiquitination, and acts through inhibition of protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 is also an inhibitor of dihydroorotate dehydrogenase (DHODH).
Targets
p53 [1]
()
Mdm2 [1]
()
DHODH [2]
()
In vitro

Tenovin-1 is a p53 activator and elevates the amount of p53 protein within 2 hr of treatment. Tenovin-1 treatment does not alter p53 mRNA levels. Tenovin-1 (10μM) protects p53 from mdm2-mediated degradation with little effect on p53 synthesis. Tenovin-1 represses cell growth, and induces apoptosis in a panel of tumor cells expressing p53. Tenovin-1 acts through inhibition of the protein-deacetylating activities of SirT1 and SirT2, two important members of the sirtuin family. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF7 cells Mk\vSpVv[3Srb36gZZN{[Xl? MWqxNEDPxE1? MmLTOkBp NF32SIFKdmirYnn0bY9vKG:oIGPpdnQyKGG|c3Xzd4VlKGG|IHnuZ5Jm[XOnIHnuJJA2OyCneIDy[ZN{cW:wIHnuJIh2dWGwIF3DSlch[2WubIOgZZQhOTBidV2gZYZ1\XJiNjDodpMh[nliV3XzeIVzdiCkbH;0eIlv\w>? MV2yNlMxPDh2OB?=
In vivo

Initial in vivo experiments indicated that tenovin-1 impairs the growth of BL2-derived tumor xenografts. [1]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: HCT116, HCT116 p53−/−, EW36, BL2, NTera2D, NTera2D-DNp53, ARN8, NHDF, SKNH-pCMV and SKNSH-DNp53.
  • Concentrations: 10 μM
  • Incubation Time: 4 days
  • Method:

    Cell viability isdetermined by trypan blue exclusion, Giemsa staining, or MTT assays.

Animal Research:

[1]

  • Animal Models: Female SCID mice injected subcutaneously with ARN8 cells suspended in matrigel.
  • Dosages: 92.5 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

DMSO 74 mg/mL
(200.28 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
15% Captisol
For best results, use promptly after mixing.

15 mg/mL

Chemical Information

Molecular Weight 369.48
Formula

C20H23N3O2S

CAS No. 380315-80-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(=O)NC1=CC=C(C=C1)NC(=S)NC(=O)C2=CC=C(C=C2)C(C)(C)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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