309271-94-1

Basic information

• Product Name: Inauhzin
• Synonyms: Inauhzin;1-Phenothiazin-10-yl-2-(9H-1,3,4,9-tetraaza-fluoren-2-ylsufanyl)-butan-1-one (Inauhzin);10-[1-Oxo-2-(2H-1,2,4-triazino[5,6-b]indol-3-ylthio)butyl]-10H-phenothiazine;Inauhzin(INZ);10-[1-Oxo-2-(2H-1,2,4-triazino[5,6-b]indol-3-ylthio)butyl]-10H-phenothiazine Inauhzin(INZ);Inauhzin 10-[1-Oxo-2-(2H-1,2,4-triazino[5,6-b]indol-3-ylthio)butyl]-10H-phenothiazine;Inauhzin, >=98%;2-((5H-[1,2,4]Triazino[5,6-b]indol-3-yl)thio)-1-(10H-phenothiazin-10-yl)butan-1-one
• CAS NO: 309271-94-1
• Molecular Formula: C25H18N5OS2
• Molecular Weight: 468.57332
• Product Categories: Inhibitors
• Mol File: 309271-94-1.mol

Chemical Properties

• Boiling Point: 773.6±70.0 °C(Predicted)
• Appearance: /
• Density: 1.50±0.1 g/cm3(Predicted)
• Solubility: ≥23.5 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
• PKA: 10.24±0.50(Predicted)
• CAS DataBase Reference: Inauhzin(CAS DataBase Reference)
• NIST Chemistry Reference: Inauhzin(309271-94-1)
• EPA Substance Registry System: Inauhzin(309271-94-1)

Safety Data

• Hazardous Substances Data: 309271-94-1(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Industry:
Inauhzin is used as an anticancer agent for its ability to inhibit SIRT1 activity and activate p53, leading to a decrease in tumor growth. This makes it a promising candidate for the development of novel cancer treatments and therapies.
Used in Cancer Research:
Inauhzin is used as a research tool to study the mechanisms of cancer cell growth and the role of SIRT1 and p53 in tumor development. Its ability to target these specific pathways can provide valuable insights into the development of new cancer treatments and therapies.

Biological Activity

inauhzin is a small-molecule inhibitor of sirt1 with ic50 value of 0.7-2μm [1].inauhzin inhibits sirt1 deacetylation activity and subsequently activates the substrate of sirt1, p53, in a dose-dependent manner. it shows an induction of acetylation of p53 and histone h3 in the k382 and k9 residues, respectively. the inhibition of sirt1 is selective. it has no significant effect on sirt2, sirt3 or hdac8 in the fluor-de-lys fluorimetric assay. since it is an activator of p53, inauhzin inhibits cell growth in different p53-containing human cancer cells including h460, h1299, a549, ht29 and wi38. the ic50 values are 5.4μm, 51.9μm, 3.2μm, 33.9μm and 85.4μm, respectively. furthermore, inauhzin induces cell apoptosis through activating p53. in the xenograft tumours derived from h460 cells, inauhzin also significantly induces p53 activity and p53-dependent apoptosis at 2μm [1].

references

[1] zhang q, zeng sx, zhang y, zhang y, ding d, ye q, meroueh so, lu h. a small molecule inauhzin inhibits sirt1 activity and suppresses tumour growth through activation of p53. embo mol med. 2012 apr;4(4):298-312.

Upstream product

• 28668-95-3 3-mercapto-5H-1,2,4-triazino[5,6-b]indole 
• 4063-35-8 2-bromo-1-(10H-phenothiazin-10-yl)butan-1-one 

Relevant articles and documents

Inauhzin analogues that induce P53, inhibit cell growth, and have antitumor activity

Inauhzin (INZ) was identified as a novel p53 activator, which selectively and efficiently suppressing tumor growth without displaying genotoxicity and with little toxicity to normal cells. A panel of INZ analogs were synthesized and evaluated their abilit

INAUHZIN ANALOGUES THAT INDUCE P53, INHIBIT CELL GROWTH, AND HAVE ANTITUMOR ACTIVITY

Inauhzin (INZ) was identified as a novel p53 activator, which selectively and efficiently suppressing tumor growth without displaying genotoxicity and with little toxicity to normal cells. A panel of INZ analogs were synthesized and evaluated their abilit