For research use only. Not for therapeutic Use.
Inauhzin（Cat No.:I003092） is a compound that acts as a cell-permeable inhibitor of SIRT1, an enzyme involved in cellular processes and aging. It exhibits an inhibitory concentration (IC50) range of 0.7-2 μM against SIRT1. By inhibiting the deacetylation activity of SIRT1, Inauhzin can reactivate p53, a tumor suppressor protein that plays a critical role in regulating cell growth and preventing cancer development. This reactivation of p53 can have implications for cancer therapy and potential therapeutic applications in diseases associated with SIRT1 dysregulation.
| Catalog Number | I003092 |
| CAS Number | 309271-94-1 |
| Synonyms | 2-((5H-[1,2,4]triazino[5,6-b]indol-3-yl)thio)-1-(10H-phenothiazin-10-yl)butan-1-one |
| Molecular Formula | C₂₅H₁₉N₅OS₂ |
| Purity | ≥95% |
| Target | Sirtuin |
| Solubility | DMSO: ≥ 21 mg/mL |
| Storage | Store at -20°C |
| IC50 | 3 uM(A549 cell); 5.4 uM (H460 cell) |
| IUPAC Name | 1-phenothiazin-10-yl-2-(5H-[1,2,4]triazino[5,6-b]indol-3-ylsulfanyl)butan-1-one |
| InChI | InChI=1S/C25H19N5OS2/c1-2-19(33-25-27-23-22(28-29-25)15-9-3-4-10-16(15)26-23)24(31)30-17-11-5-7-13-20(17)32-21-14-8-6-12-18(21)30/h3-14,19H,2H2,1H3,(H,26,27,29) |
| InChIKey | VHUOXERIKQWIJE-UHFFFAOYSA-N |
| SMILES | CCC(C(=O)N1C2=CC=CC=C2SC3=CC=CC=C31)SC4=NC5=C(C6=CC=CC=C6N5)N=N4 |
| Reference | </br>1:Determination of Maximum Tolerated Dose and Toxicity of Inauhzin in Mice. Zhang Q, Zeng SX, Lu H.Toxicol Rep. 2015;2:546-554. PMID: 26167454 Free PMC Article</br>2:Inauhzin(c) inactivates c-Myc independently of p53. Jung JH, Liao JM, Zhang Q, Zeng S, Nguyen D, Hao Q, Zhou X, Cao B, Kim SH, Lu H.Cancer Biol Ther. 2015;16(3):412-9. doi: 10.1080/15384047.2014.1002698. PMID: 25692307 Free PMC Article</br>3:The role of IMP dehydrogenase 2 in Inauhzin-induced ribosomal stress. Zhang Q, Zhou X, Wu R, Mosley A, Zeng SX, Xing Z, Lu H.Elife. 2014 Oct 27;3. doi: 10.7554/eLife.03077. PMID: 25347121 Free PMC Article</br>4:Inauhzin sensitizes p53-dependent cytotoxicity and tumor suppression of chemotherapeutic agents. Zhang Y, Zhang Q, Zeng SX, Hao Q, Lu H.Neoplasia. 2013 May;15(5):523-34. PMID: 23633924 Free PMC Article</br>5:Global effect of inauhzin on human p53-responsive transcriptome. Liao JM, Zeng SX, Zhou X, Lu H.PLoS One. 2012;7(12):e52172. doi: 10.1371/journal.pone.0052172. Epub 2012 Dec 21. PMID: 23284922 Free PMC Article</br>6:Structure and activity analysis of Inauhzin analogs as novel antitumor compounds that induce p53 and inhibit cell growth. Zhang Q, Ding D, Zeng SX, Ye QZ, Lu H.PLoS One. 2012;7(10):e46294. doi: 10.1371/journal.pone.0046294. Epub 2012 Oct 24. PMID: 23115626 Free PMC Article</br>7:Inauhzin and Nutlin3 synergistically activate p53 and suppress tumor growth. Zhang Y, Zhang Q, Zeng SX, Zhang Y, Mayo LD, Lu H.Cancer Biol Ther. 2012 Aug;13(10):915-24. doi: 10.4161/cbt.20844. Epub 2012 Aug 1. PMID: 22785205 Free PMC Article</br>8:A small molecule Inauhzin inhibits SIRT1 activity and suppresses tumour growth through activation of p53. Zhang Q, Zeng SX, Zhang Y, Zhang Y, Ding D, Ye Q, Meroueh SO, Lu H.EMBO Mol Med. 2012 Apr;4(4):298-312. doi: 10.1002/emmm.201100211. Epub 2012 Feb 13. PMID: 22331558 Free PMC Article |
