ALOX5 stabilizer-1
ALOX5 stabilizer-1 is an arachidonate 5-lipoxygenase (ALOX5) stabilizer with a Kd of 7.26 μM. ALOX5 stabilizer-1 inhibits β-catenin protein levels and then suppresses STAT3 signal pathway. ALOX5 stabilizer-1 induces lung cancer cells apoptosis, inhibited cell migration and proliferation. ALOX5 stabilizer-1 can used for the study of non-small cell lung cancer (NSCLC).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C32H32N4O5
- Molecular Weight:552.62
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
STAT3 |
In Vitro
ALOX5 stabilizer-1 (Compound 10d) (72 h) inhibits NCI-H820 cell proliferation with an IC50 of 0.11 μM and shows weaker toxicity against 3T3 cells with an IC50 of 0.48 μM [1].
ALOX5 stabilizer-1 (0-0.2 μM, 10 d) inhibits colony formation of with NCI-H820 cells a dose-dependent manner[1].
ALOX5 stabilizer-1 (0-0.2 μM, 48 h) inhibits NCI-H820 cell migration and induces cell apoptosis[1].
ALOX5 stabilizer-1 (0-0.2 μM, 48 h) directly targets ALOX5 protein and enhances protein stability, then inhibites β-catenin protein levels and eventually suppressed STAT3 signal pathway in NCI-H820 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H820 cells
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Concentration:0, 0.05, 0.1 and 0.2 μM
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Incubation Time:48 h
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Result:Obviously inhibited migration in dose-dependent manner.
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Cell Line:NCI-H820 cells
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Concentration:0, 0.05, 0.1 and 0.2 μM
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Incubation Time:48 h
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Result:Increased the percentage of apoptosis.
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Cell Line:NCI-H820 cells
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Concentration:0, 0.02, 0.05, 0.1 and 0.2 μM
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Incubation Time:48 h
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Result:Significantly decreased the expression of anti-apoptotic proteins Bcl-2 and Mcl-1 while increased the expression of apoptosis-related protein Bax in a dose-dependent manner.
Was directly bound to ALOX5 protein.
Inhibited both the nuclear translocation and protein levels of β-catenin.
Reduced the levels of STAT3 and p-STAT3.
Chemical Information
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Molecular Weight 552.62
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Formel C32H32N4O5
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SMILES
C[C@@]12CC/C=C(CN3C=C(N=N3)COC4=CC=C(C=C4)C(/C=C/C5=CC=CN=C5)=O)\CC[C@@H]6[C@H](OC(C6=C)=O)[C@H]1O2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 50 mg/mL (90.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
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 (4.52 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.52 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
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.
Reinheit & Dokumentation
Verweise
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.8096 mL | 9.0478 mL | 18.0956 mL | 45.2390 mL |
| 5 mM | 0.3619 mL | 1.8096 mL | 3.6191 mL | 9.0478 mL | |
| 10 mM | 0.1810 mL | 0.9048 mL | 1.8096 mL | 4.5239 mL | |
| 15 mM | 0.1206 mL | 0.6032 mL | 1.2064 mL | 3.0159 mL | |
| 20 mM | 0.0905 mL | 0.4524 mL | 0.9048 mL | 2.2620 mL | |
| 25 mM | 0.0724 mL | 0.3619 mL | 0.7238 mL | 1.8096 mL | |
| 30 mM | 0.0603 mL | 0.3016 mL | 0.6032 mL | 1.5080 mL | |
| 40 mM | 0.0452 mL | 0.2262 mL | 0.4524 mL | 1.1310 mL | |
| 50 mM | 0.0362 mL | 0.1810 mL | 0.3619 mL | 0.9048 mL | |
| 60 mM | 0.0302 mL | 0.1508 mL | 0.3016 mL | 0.7540 mL | |
| 80 mM | 0.0226 mL | 0.1131 mL | 0.2262 mL | 0.5655 mL |
ALOX5 stabilizer-1 Related Classifications
HY-175634 Related Classifications
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