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Inauhzin Sirtuin inhibitor

Cat.No.S6744

Inauhzin is a cell-permeable SIRT1 inhibitor with an IC50 of 0.7-2 μM and reactivates p53 by inhibiting SIRT1 deacetylation activity.
Inauhzin Sirtuin inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 469.58

Quality Control

Batch: S674401 DMSO]94 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.66%
99.66

Chemical Information, Storage & Stability

Molecular Weight 469.58 Formula

C25H19N5OS2

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 309271-94-1 -- Storage of Stock Solutions

Synonyms N/A Smiles CCC(C(=O)N1C2=CC=CC=C2SC3=CC=CC=C31)SC4=NC5=C(C6=CC=CC=C6N5)N=N4

Solubility

In vitro
Batch:

DMSO : 94 mg/mL ( (200.17 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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.
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.

Mechanism of Action

Targets/IC50/Ki
SIRT1 [2]
p53 [1]
In vitro

Inauhzin (INZ) is a potent p53 activator and mediates p53-dependent cytotoxicity. This compound inhibits cell proliferation by triggering both apoptosis and senescence in p53-containning cells, though it predominantly induces p53-dependent apoptosis. It is able to prevent p53 from MDM2-mediated ubiquitylation and proteasomal degradation and protects p53 without either directly inhibiting MDM2 activity towards p53 or interfering with MDMX/MDM2–p53 interaction. This chemical induces acetylation of p53, but not tubulin, in cells[1]. It is a (sub)micromolar SIRT1i selective over SIRT2/3[2].

In vivo

Inauhzin (INZ) has good tumour tissue penetration and is able to inhibit tumour growth by inducing p53[1].

References

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