Home Apoptosis p53 activator - Sirtuin inhibitor - Dehydrogenase inhibitor Tenovin-1 For research use only.

Tenovin-1

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

Tenovin-1 Chemical Structure

CAS No. 380315-80-0

Purity & Quality Control

Batch: S800001 DMSO]74 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.82%
99.82

Tenovin-1 Related Products

Signaling Pathway

p53 Signaling Pathways

p53 Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF7 cells Function assay 10 μM 6 h Inhibition of SirT1 assessed as increase in p53 expression in human MCF7 cells at 10 uM after 6 hrs by Western blotting 22304848
Click to View More Cell Line Experimental Data

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
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 Research 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.
In Vivo
In vivo

Initial in vivo experiments indicated that tenovin-1 impairs the growth of BL2-derived tumor xenografts. [1]
Animal Research Animal Models Female SCID mice injected subcutaneously with ARN8 cells suspended in matrigel.
Dosages 92.5 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 369.48 Formula

C20H23N3O2S
CAS No. 380315-80-0 SDF Download Tenovin-1 SDF
Smiles CC(=O)NC1=CC=C(C=C1)NC(=S)NC(=O)C2=CC=C(C=C2)C(C)(C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 74 mg/mL ( (200.28 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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In vivo Formulation Calculator

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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.

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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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