Inauhzin (Synonyms: INZ) |
| Catalog No.GC14755 |
SIRT1 inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 309271-94-1
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment [1]: | |
|
Cell lines |
H460, H1299, A549, HT29 and WI38 |
|
Preparation method |
The solubility of this compound in DMSO is > 23.5 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
2μM, 18h |
|
Applications |
Inauhzin dose-dependently inhibited cell growth in different p53-containing human cancer cells including H460, H1299, A549, HT29 and WI38. Inauhzin effectively reactivated p53 by inhibiting SIRT1 activity, promoted p53-dependent apoptosis of human cancer cells without causing apparently genotoxic stress. Moreover, INZ stabilized p53 by increasing p53 acetylation and preventing MDM2-mediated ubiquitylation of p53 in cells. INZ inhibited cell proliferation, induced senescence and tumour-specific apoptosis. |
| Animal experiment [1]: | |
|
Animal models |
Female SCID mice bearing H460 or HCT116 xenografts |
|
Dosage form |
Intraperitoneal injection, 18h, 2μM |
|
Application |
Inauhzin repressed 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. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1]. Zhang Q, Zeng S X, Zhang Y, et al. A small molecule Inauhzin inhibits SIRT1 activity and suppresses tumour growth through activation of p53[J]. EMBO molecular medicine, 2012, 4(4): 298-312. | |
| Cas No. | 309271-94-1 | SDF | |
| Synonyms | INZ | ||
| Chemical Name | 2-((5H-[1,2,4]triazino[5,6-b]indol-3-yl)thio)-1-(10H-phenothiazin-10-yl)butan-1-one | ||
| Canonical SMILES | CCC(SC1=NC2=C(N=N1)C3=CC=CC=C3N2)C(N4C5=CC=CC=C5SC6=CC=CC=C64)=O | ||
| Formula | C25H19N5OS2 | M.Wt | 469.58 |
| Solubility | ≥ 23.5mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1296 mL | 10.6478 mL | 21.2956 mL |
| 5 mM | 0.4259 mL | 2.1296 mL | 4.2591 mL |
| 10 mM | 0.213 mL | 1.0648 mL | 2.1296 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 1 reference(s) in Google Scholar.)
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