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Product name : Inauhzin
Item : CR1805
Price : 200mg, $845; 500mg, $1485
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Additional Information :  We offer significant discount for bulky quantity order,Please ask price and availability of other quantities
CAS : 309271-94-1
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Details:
 Chemical Information
M.Wt 469.58 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C25H19N5OS2
CAS No 309271-94-1
Solubility

DMSO



Biological Activity of Inauhzin

 

Inauhzin(INZ) is a novel small molecule that effectively reactivates p53 by inhibiting SIRT1 activity, promotes p53-dependent apoptosis of human cancer cells without causing apparently genotoxic stress(IC50=3 uM, in A549 cell).
IC50 value: 3 uM(A549 cell); 5.4 uM (H460 cell) [1]
Target: SIRT1
in vitro: Inauhzin effectively reactivates p53 by inhibiting SIRT1 activity, promotes p53-dependent apoptosis of human cancer cells without causing apparently genotoxic stress. Moreover, INZ stabilizes p53 by increasing p53 acetylation and preventing MDM2-mediated ubiquitylation of p53 in cells, though not directly in vitro. Remarkably, INZ inhibits cell proliferation, induces senescence and tumour-specific apoptosis [1].
in vivo: represses the growth of xenograft tumours derived from p53-harbouring H460 and HCT116 cells without causing apparent toxicity to normal tissues and the tumour-bearing SCID mice [1].
 

 

[1]. Zhang Q, et al. A small molecule Inauhzin inhibits SIRT1 activity and suppresses tumour growth through activation of p53. EMBO Mol Med. 2012 Apr;4(4):298-312.
Abstract
Although ~50% of all types of human cancers harbour wild-type TP53, this p53 tumour suppressor is often deactivated through a concerted action by its abnormally elevated suppressors, MDM2, MDMX or SIRT1. Here, we report a novel small molecule Inauhzin (INZ) that effectively reactivates p53 by inhibiting SIRT1 activity, promotes p53-dependent apoptosis of human cancer cells without causing apparently genotoxic stress. Moreover, INZ stabilizes p53 by increasing p53 acetylation and preventing MDM2-mediated ubiquitylation of p53 in cells, though not directly in vitro. Remarkably, INZ inhibits cell proliferation, induces senescence and tumour-specific apoptosis, and represses the growth of xenograft tumours derived from p53-harbouring H460 and HCT116 cells without causing apparent toxicity to normal tissues and the tumour-bearing SCID mice. Hence, our study unearths INZ as a novel anti-cancer therapeutic candidate that inhibits SIRT1 activity and activates p53.


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