Home Epigenetics Sirtuin inhibitor Inauhzin For research use only.

Inauhzin

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

Inauhzin Chemical Structure

Inauhzin Chemical Structure

CAS: 309271-94-1

Selleck's Inauhzin has been cited by 2 publications

Purity & Quality Control

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

Inauhzin Related Products

Signaling Pathway

Sirtuin Signaling Pathways

Sirtuin Signaling Pathway

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Biological Activity

Description Inauhzin is a cell-permeable SIRT1 inhibitor with an IC50 of 0.7-2 μM and reactivates p53 by inhibiting SIRT1 deacetylation activity.
Targets
SIRT1 [2] p53 [1]
In vitro
In vitro

Inauhzin (INZ) is a potent p53 activator and mediates p53-dependent cytotoxicity. INZ inhibits cell proliferation by triggering both apoptosis and senescence in p53-containning cells, though it predominantly induces p53-dependent apoptosis. INZ 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. INZ induces acetylation of p53, but not tubulin, in cells[1]. Inauhzin is a (sub)micromolar SIRT1i selective over SIRT2/3[2].
Cell Research Cell lines human lung cancer H460, A549, H1299, colon cancer HCT116, HT29, osteosarcoma U2OS and SJSA, breast cancer MCF7, ovarian cancer A2780, IGROV1 and SKOV3 and glioma U87 and U373 cells, as well as human embryonic fibroblast WI-38 and normal human fibroblast (NHF) cells
Concentrations 0-10 μM
Incubation Time 18 h
Method

--
In Vivo
In vivo

Inauhzin (INZ) has good tumour tissue penetration and is able to inhibit tumour growth by inducing p53[1].
Animal Research Animal Models SCID mice with H460 xenograft tumours
Dosages 30 mg/kg
Administration IP

Chemical Information & Solubility

Molecular Weight 469.58 Formula

C25H19N5OS2
CAS No. 309271-94-1 SDF --
Smiles CCC(C(=O)N1C2=CC=CC=C2SC3=CC=CC=C31)SC4=NC5=C(C6=CC=CC=C6N5)N=N4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble


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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.

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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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