Home Apoptosis p53 activator - Sirtuin inhibitor - Dehydrogenase inhibitor Tenovin-1

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Tenovin-1 p53 activator

Cat.No.S8000

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

Chemical Structure

Molecular Weight: 369.48

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S800001 DMSO]250 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.82%
99.82

Cell Culture, Treatment & Working Concentration

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
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight 369.48 Formula

C20H23N3O2S

 Storage (From the date of receipt)
CAS No. 380315-80-0 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC(=O)NC1=CC=C(C=C1)NC(=S)NC(=O)C2=CC=C(C=C2)C(C)(C)C

Solubility

In vitro
Batch:

DMSO : 250 mg/mL (676.62 mM) Ultrasonicated;
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Mechanism of Action

Targets/IC50/Ki
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. This compound treatment does not alter p53 mRNA levels. It (10μM) protects p53 from mdm2-mediated degradation with little effect on p53 synthesis. This chemical represses cell growth, and induces apoptosis in a panel of tumor cells expressing p53. It acts through inhibition of the protein-deacetylating activities of SirT1 and SirT2, two important members of the sirtuin family. [1]
In vivo

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

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