Inauhzin
Based on 3 publication(s) in Google Scholar
Inauhzin is a dual SirT1/IMPDH2 inhibitor, and acts as an activator p53, used in the research of cancer.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.46%
- CAS. Nr.: 309271-94-1
- Formel: C25H19N5OS2
- Molecular Weight:469.58
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Inauhzin
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Biologische Aktivität
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SIRT1 |
MDM-2/p53 |
IMPDH2 |
Inauhzin (10 μM) induces p53 levels as effectively as actinomycin D (10 nM), and mediates p53-dependent cytotoxicity through its specific functional groups in human lung carcinoma H460 cells. Inauhzin (2 μM) induces p53 level and activity as well as p53-dependent apoptosis. Inauhzin also stabilizes p53 and inhibits its ubiquitylation. Inauhzin induces acetylation of p53 in H460 cells, but not tubulin, which is affected by knockdown of SIRT1[1]. Inauhzin (0-2 μM) significantly enhances the expression level and activity of p53 in HCT116p53+/+ cells and enhances the expression level and activity of p53 in H460 cells in a dose-dependent manner. Inauhzin and Nutlin-3 demonstrate synergistic cytotoxicity in the Nutlin-3 low-sensitive cells. Inauhzin and Nutlin-3 synergistically induce p53-dependent apoptosis[2]. Inauhzin targets both SirT1 and IMP dehydrogenase 2 (IMPDH2), and acts as a potent p53 activator[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 309271-94-1
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Appearance Solid
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Molecular Weight 469.58
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Formel C25H19N5OS2
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Color Light yellow to yellow
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SMILES
CCC(SC1=NN=C2C(NC3=C2C=CC=C3)=N1)C(N4C5=C(C=CC=C5)SC6=CC=CC=C46)=O
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Synonyms
INZ
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Nat Commun
Selective inhibition of cancer cell self-renewal through a Quisinostat-histone H1.0 axis. [Abstract]2020 Apr 14;11(1):1792. PMID: 32286289 -
J Exp Clin Cancer Res
Pyrotinib targeted EGFR/GRP78 mediated cell apoptosis in high EGFR gene copy number gastric cancer. [Abstract]2025 Aug 19;44(1):245. PMID: 40830980 -
Proc Natl Acad Sci U S A
2019 Feb 19;116(8):2961-2966. PMID: 30718431
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (212.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.32 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
The cell counting kit is used to assess cell growth. Cell suspensions are seeded at 5000 cells per well in 96-well culture plates and incubated overnight at 37°C. Compounds are added into the plates and incubated at 37°C for 72 h. Cell growth inhibition is determined by adding WST-8 at a final concentration of 10% to each well, and the absorbance of the samples is measured at 450 nm using a Microplate Reader[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Five-weeks-old female SCID mice are housed in a BSL2 environment. Mice are subcutaneously inoculated with 5×106 H460 or 3×106 HCT116 cells. Tumour growth is monitored every other day with electronic digital calipers in two dimensions. Tumour volume is calculated with the formula: tumour volume (mm3) = (length × width2)/2. When the mean tumour volume reaches approximately 100 mm3 after 7-9 days, animals are dosed by i.p. injection with vehicle (5% DMSO) or Inauhzin. Inhibition of tumour growth is calculated on the last day of treatment. To detect p53 activation in vivo, tumours are harvested and disrupted in RIPA buffer containing a protease inhibitor mixture. Tumour lysates are analysed by IB. Cell proliferation in tumours is assessed by BrdU labeling followed by Immunostaining. 200 mg/kg body weight of BrdU is administrated to mice via i.p. injection 2 h before mice are sacrificed. Apoptosis is examined by TUNEL staining, using the Fluorescein In situ cell death detection kit[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[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. [Content Brief]
[2]. Zhang Y, et al. Inauhzin and Nutlin3 synergistically activate p53 and suppress tumor growth. Cancer Biol Ther. 2012 Aug;13(10):915-24. [Content Brief]
[3]. Nguyen D, et al. Reviving the guardian of the genome: Small molecule activators of p53. Pharmacol Ther. 2017 Oct;178:92-108. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1296 mL | 10.6478 mL | 21.2956 mL | 53.2391 mL |
| 5 mM | 0.4259 mL | 2.1296 mL | 4.2591 mL | 10.6478 mL | |
| 10 mM | 0.2130 mL | 1.0648 mL | 2.1296 mL | 5.3239 mL | |
| 15 mM | 0.1420 mL | 0.7099 mL | 1.4197 mL | 3.5493 mL | |
| 20 mM | 0.1065 mL | 0.5324 mL | 1.0648 mL | 2.6620 mL | |
| 25 mM | 0.0852 mL | 0.4259 mL | 0.8518 mL | 2.1296 mL | |
| 30 mM | 0.0710 mL | 0.3549 mL | 0.7099 mL | 1.7746 mL | |
| 40 mM | 0.0532 mL | 0.2662 mL | 0.5324 mL | 1.3310 mL | |
| 50 mM | 0.0426 mL | 0.2130 mL | 0.4259 mL | 1.0648 mL | |
| 60 mM | 0.0355 mL | 0.1775 mL | 0.3549 mL | 0.8873 mL | |
| 80 mM | 0.0266 mL | 0.1331 mL | 0.2662 mL | 0.6655 mL | |
| 100 mM | 0.0213 mL | 0.1065 mL | 0.2130 mL | 0.5324 mL |